Category: 104-01-8

Xi, Wenli published the artcileIdentification of Novel 4′-O-Demethyl-epipodophyllotoxin Derivatives as Antitumor Agents Targeting Topoisomerase II, Recommanded Product: 4-Methoxyphenylacetic acid, the main research area is demethylepipodophyllotoxin preparation antitumor topoisomerase II inhibitor; 4′-O-demethyl-epipodophyllotoxin; antitumor agent; topoisomerase II.

C4 variation of 4′-O-demethyl-epipodophyllotoxin (DMEP) I is an effective approach to optimize the antitumor spectra of this compound class. Accordingly, two series of novel DMEP derivatives were synthesized, and as expected, the antitumor spectra of these derivatives varied with different C4 substituents. Notably, most compounds showed significant inhibition against the etoposide (2)-resistant KBvin cells. Four of the compounds I (R = [4-[3-(dimethylamino)propanamido]phenyl]aminyl, (4-[3-[benzyl(methyl)amino]propanamido]phenyl)aminyl, [1-[(4-fluorophenyl)methyl]piperidin-4-yl]amidyl and 3-[benzyl(methyl)amino]propanamidyl) induced protein-linked DNA break (PLDB) levels higher than those of GL-331 I (R = (4-nitrophenyl)aminyl), and are assumed to be topoisomerase II (topo II) poisons more potent than I (R = (4-nitrophenyl)aminyl) and 2. Compound I (R = 3-[benzyl(methyl)amino]propanamidyl), a potent topo II poison highly effective against KBvin cells, was further evaluated with a panel of tumor cells and was most active against HepG2. This compound also exhibited apparent in vivo antitumor efficacy in hepatoma 22 (H22) mouse model. The results indicated that C4 derivation of DMEP is a feasible approach to identify potent topo II inhibitors with optimized antitumor profiles.

Molecules published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Recommanded Product: 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Li, Yingfen published the artcileOne-pot synthesis of benzimidazole-pyrazines and their anticancer activities, SDS of cas: 104-01-8, the main research area is fused benzimidazole pyrazine one pot preparation antitumor human.

The skeleton of fused benzimidazole-pyrazines I (R1 = Ph, 4-ClC6H4; R2 = Ph, CH2(4-MeOC6H4), CH2(4-ClC6H4), CH2(3,4-(Cl)2C6H3)) was constructed via an Ugi/deprotection/cyclization (UDC) and hydroamination cascade reaction. This four-step reaction was carried out in a one-pot procedure with only one-time column chromatog. purification The representative compound I (R1 = Ph; R2 = CH2(4-ClC6H4)) exhibited 67% cell growth inhibitory activity against human breast cancer cell line MDA-MB-453 at the concentration of 10μM.

Journal of Heterocyclic Chemistry published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, SDS of cas: 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Yao, Hong published the artcileDesign, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors, SDS of cas: 104-01-8, the main research area is truncated deguelin synthesis SAR mol docking breast lung antitumor; deguelin truncated derivative heat shock protein inhibitor antitumor; antitumor truncated deguelin apoptosis inducer cell cycle arrest; cell migration inhibitor truncated deguelin derivative antitumor; Anticancer; Deguelin; Heat shock protein 90; Structure simplification.

A series of novel B- and C-rings truncated deguelin derivatives have been designed and synthesized in the present study as heat shock protein 90 (Hsp90) inhibitors. The synthesized compounds exhibited micromolar antiproliferative potency toward a panel of human cancer cell lines. Their structure-activity relationships (SARs) were investigated in a systematic manner. Compound I was identified to have high Hsp90 binding potency (60 nM) and caused degradation of client proteins through ubiquitin proteasome system. Further biol. studies showed that compound I induced a dose-dependent S and G2-phase cell cycle arrest on human breast cancer MCF-7 cells. Flow cytometry and Western blot analyses confirmed that compound I caused apoptosis of MCF-7 cells. In addition, compound I showed much potent inhibition on the migration and invasion of MCF-7 cells. Taken together, these results suggest that I might be a promising lead compound for further development of Hsp90 inhibitors.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, SDS of cas: 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Avvaru, Stephen P. published the artcileSynthesis and Anticancer Activity of Thiadiazole Containing Thiourea, Benzothiazole and Imidazo[2,1-b][1,3,4]thiadiazole Scaffolds, SDS of cas: 104-01-8, the main research area is thiadiazole thiourea benzothiazole imidazothiadiazole scaffold anticancer activity; 1; 1-b][1; 3; 4-thiadiazole; 4]thiadiazole; anticancer activity; aromatase; benzothiazole; docking.; imidazo[2; letrozole.

A great array of nitrogen-containing heterocyclic rings were being extensively explored for their functional versatility in the field of medicine, especially in anticancer research. 1,3,4- thiadiazole is one of such heterocyclic rings with promising anticancer activity against several cancer cell lines, inhibiting diverse biol. targets. The 1,3,4-thiadiazole, when equipped with other heterocyclic scaffolds, has displayed enhanced anticancer properties. The thiourea, benzothiazole, imidazo[2,1,b][1,3,4]-thiadiazoles are such potential scaffolds with promising anticancer activity. A new series of 5-substituted-1,3,4-thiadiazoles linked with Ph thiourea, benzothiazole and 2,6-disubstituted imidazo[2,1-b][1,3,4]thiadiazole derivatives were synthesized and tested for invitro anticancer activity on various cancer cell lines. The National Cancer Institute′s preliminary anticancer screening results showed compounds 4b and 5b having potent antileukemic activity. Compound 4b selectively showed 32 percent lethality on Human Leukemia-60 cell line. The docking studies of the derivatives on aromatase enzyme (Protein Data Bank: 3S7S) have shown reversible interactions at the active site with good docking scores comparable to Letrozole and Exemestane. Furthermore, the selected derivatives were tested for anticancer activity on HeLa cell line based on the mol. docking studies. Compounds 4b and 5b showed effective inhibition equivalent to Letrozole. These preliminary biol. screening studies have given pos. anticancer activity for these new classes of derivatives An addnl. research study like the mechanism of action of the anticancer activity of this new class of compounds is necessary. These groundwork studies illuminate a future pathway for research of this class of compounds enabling the discovery of potent antitumor agents.

Medicinal Chemistry (Sharjah, United Arab Emirates) published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, SDS of cas: 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Choodamani, B. published the artcileSynthesis, Molecular Docking and Preliminary Antileukemic Activity of 4-Methoxybenzyl Derivatives Bearing Imidazo[2,1-b][1,3,4]thiadiazole, Name: 4-Methoxyphenylacetic acid, the main research area is methoxybenzyl derivative mol docking antitimor agent; TGF beta receptor kinase; cytotoxicity; imidazothiadiazole; levamisole; melphalan.

In this study, we synthesized 22 compounds in a series with various substitution on imidazo[2,1-b][1,3,4]thiadiazole. The potential cytotoxic activity of these compounds investigated in leukemia cell lines by Differential Nuclear Staining (DNS). Our results identified two compounds, 2-(4-methoxybenzyl)-6-(2-oxo-2H-chromen-3-yl)imidazo[2,1-b][1,3,4]thiadiazol-5-yl thiocyanate and 6-(4-chlorophenyl)-2-(4-methoxybenzyl)imidazo[2,1-b][1,3,4]thiadiazole-5-carbaldehyde, exhibited the most cytotoxic effect against murine leukemia cells (L1210), human T-lymphocyte cells (CEM) and human cervix carcinoma cells (HeLa) with IC50 values ranging between 0.79 and 1.6μM. The results indicate that 2-(4-methoxybenzyl)-6-(2-oxo-2H-chromen-3-yl)imidazo[2,1-b][1,3,4]thiadiazol-5-yl thiocyanate is inducing phosphatidylserine externalization and caspase-3 activation which are both a hallmark of apoptosis. Docking studies showed that 2-(4-methoxybenzyl)-6-(2-oxo-2H-chromen-3-yl)imidazo[2,1-b][1,3,4]thiadiazol-5-yl thiocyanate binds within the active sites of transforming growth factor beta (TGF-β) type I receptor kinase domain by strong hydrogen binding and hydrophobic interactions.

Chemistry & Biodiversity published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Name: 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Liew, Lydia P. published the artcileHypoxia-Activated Prodrugs of PERK Inhibitors, Formula: C9H10O3, the main research area is hypoxia prodrug drug delivery PERK kinase inhibitor antitumor; drug delivery; hypoxia; kinase inhibitor; nitroimidazole; prodrug.

Tumor hypoxia plays an important role in tumor progression and resistance to therapy. Under hypoxia unfolded proteins accumulate in the endoplasmic reticulum (ER) and this stress is relieved through the protein kinase R-like ER kinase (PERK) signaling arm of the unfolded protein response (UPR). Targeting the UPR through PERK kinase inhibitors provides tumor growth inhibition, but also elicits on-mechanism normal tissue toxicity. Hypoxia presents a target for tumor-selective drug delivery using hypoxia-activated prodrugs. We designed and prepared hypoxia-activated prodrugs of modified PERK inhibitors using a 2-nitroimidazole bioreductive trigger. The new inhibitors retained PERK kinase inhibitory activity and the corresponding prodrugs were strongly deactivated. The prodrugs were able to undergo fragmentation following radiolytic reduction, or bioreduction in HCT116 cells, to release their effectors, albeit inefficiently. We examined the effects of the prodrugs on PERK signaling in hypoxic HCT116 cells. This study has identified a 2-substituted nitroimidazole carbamate prodrug with potential to deliver PERK inhibitors in a hypoxia-selective manner.

Chemistry – An Asian Journal published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Formula: C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Liu, Wenjing published the artcileDesign, synthesis and biological evaluation of novel 4-(4-methoxynaphthalen-1-yl)-5-arylpyrimidin-2-amines as tubulin polymerization inhibitors, SDS of cas: 104-01-8, the main research area is methoxynaphthalenylarylpyrimidinamine preparation tubulin polymerization inhibitor antitumor; anticancer; naphthalene; pyrimidine; tubulin polymerization inhibitor.

A novel series of 4-(4-methoxynaphthalen-1-yl)-5-arylpyrimidin-2-amines I (R = 4-OEt, 4-Me, 4-Cl, etc.) were designed, synthesized, and evaluated for their anticancer activities. Most of the synthesized compounds exhibited moderate to high antiproliferative activity in comparison to the standard drug cisplatin. Among them, I (R = 4-OEt) was found to be the most active on MCF-7 and HepG2 cancer cell lines, with IC50 values of 3.77 +/= 0.36 and 3.83 +/= 0.26μM, resp. Further mechanism study shown that I (R = 4-OEt) potently inhibited tubulin polymerization, induced cell cycle arrest at G2/M phase and cell apoptosis in MCF-7 cell line. Furthermore, mol. modeling study suggested that I (R = 4-OEt) probably binds to the colchicine site of tubulin.

Chemical & Pharmaceutical Bulletin published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, SDS of cas: 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Dong, Junmin published the artcileDesign, synthesis and biological evaluation of exiguamine A analogues as IDO1 inhibitors, SDS of cas: 104-01-8, the main research area is exiguamine A preparation SAR mol docking antitumor indoleamine dioxygenase; Cancer immunotherapy; Exiguamine A; Indoleamine 2,3-dioxygenase 1.

A series of exiguamine A analogs were designed and synthesized via 15 steps. Their inhibitory activities against IDO1 were tested and the structure-activity relationships were studied. Most compounds exhibited potent IDO1 inhibitory activities with IC50 values at the level of 10-7-10-8 M. Compound I was the most potent IDO1 inhibitor with an IC50 value of 65.3 nM, which was comparable with the pos. control drug epacadostat (IC50 = 46 nM). Moreover, compound I showed higher selectivity for IDO1 over tryptophan 2,3-dioxygenase (TDO) and no cytotoxicity at its effective concentration, rending it justifiable for further optimization and evaluation.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, SDS of cas: 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Li, Xinyu published the artcileSynthesis and biological evaluation of 3-aryl-quinoline derivatives as anti-breast cancer agents targeting ERα and VEGFR-2, Related Products of isoquinoline, the main research area is antitumor arylquinoline estrogen receptor alpha VEGFR 2 multi target; arylquinoline SAR anti breast cancer multi target; Anti-breast cancer; Estrogen receptor; Multi target; VEGFR-2.

Selective estrogen receptor modulators(SERMs) are a series of important small mol. compounds to modulate the estrogen receptor, such as tamoxifen. Although these drugs have shown great benefits in the treatment of breast cancer, the risk of endometrial cancer and endocrine resistance restrict their use. The reasonable designing of multi-target drugs can decrease the side effects and improve the tolerance of antineoplastic agents. Studies have identified that VEGFR-2 plays a pivotal role in tumor angiogenesis and drug resistance. Besides, a combination of Tamoxifen and a low dose of a VEGFR-2 inhibitor was reported to maximize therapeutic efficacy as well as to retard SERM resistant tumor growth. In this work, a series of 3-aryl-quinoline derivatives were designed to target ERα and VEGFR-2 to eliminate the disadvantages of SERMs. We identified that compounds I [R1 = H, R2 = MeO; R1 = MeO, R2 = H] displayed highly ER binding affinities as well as relative intensity VEGFR-2 inhibitory activities. Moreover, these two compounds exhibited excellent anti-proliferative activities against MCF-7 and HUVEC cell lines with low micromolar IC50 (1-8 μM). A further study confirmed that compound I [R1 = MeO, R2 = H] can reduce the expression of PgR mRNA, arrest cell cycle in MCF-7 breast cancer cells, and restrain the cell migration. Overall, based on the biol. activities data, I [R1 = MeO, R2 = H] can be chosen as a potential anti-cancer lead compound for further studying.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Related Products of isoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Destro, Gianluca published the artcileTransition-Metal-Free Carbon Isotope Exchange of Phenyl Acetic Acids, COA of Formula: C9H10O3, the main research area is transition metal free carbon isotope exchange phenylacetic acid; carbon dioxide; carbon-11; carbon-14; isotope exchange; isotope labeling.

A transition-metal-free carbon isotope exchange procedure on Ph acetic acids is described. Utilizing the universal precursor CO2, this protocol allows the carbon isotope to be inserted into the carboxylic acid position, with no need of precursor synthesis. This procedure enabled the labeling of 15 pharmaceuticals and was compatible with carbon isotopes [14C] and [13C]. A proof of concept with [11C] was also obtained with low molar activity valuable for distribution studies.

Angewandte Chemie, International Edition published new progress about Exchange reaction. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, COA of Formula: C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem