Day: December 6, 2022

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

Subtelna, Ivanna published the artcile5-Arylidene-2-(4-hydroxyphenyl)aminothiazol-4(5H)-ones with selective inhibitory activity against some leukemia cell lines, COA of Formula: C9H10O3, the main research area is anticancer antileukemic leukemia 2imino4thiazolidinone; 2-imino-4-thiazolidinones; anticancer activity; antileukemic activity; leukemia cell lines.

The data on the pharmacol. of 4-thiazolidinones showed that 5-ene-2-(imino)amino-4-thiazolidinones are likely to comprise one of the most promising groups of compounds possessing anticancer properties. A series of 5-arylidene-2-(4-hydroxyphenyl)aminothiazol-4(5H)-ones was designed, synthesized, and studied against 10 leukemia cell lines, including the HL-60, Jurkat, K-562, Dami, KBM-7, and some Ba/F3 cell lines. The structure-activity relationship anal. shows that almost all tested 5-arylidene-2-(4-hydroxyphenyl)aminothiazol-4(5H)-ones were characterized by IC50 values lower or comparable to that of the control drug chlorambucil. Among the tested compounds, (5Z)-5-(2-methoxybenzylidene)- (12), (5Z)-(2-ethoxybenzylidene)- (21), (5Z)-5-(2-benzyloxybenzylidene)- (25), and (5Z)-5-(2-allyloxybenzylidene)-2-(4-hydroxyphenylamino)thiazol-4(5H)-ones (28) possessed the highest antileukemic activity at submicromolar concentrations (IC50 = 0.10-0.95μM).

Archiv der Pharmazie (Weinheim, Germany) published new progress about Antitumor agents. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, COA of Formula: C9H10O3.

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

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

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

Cai, Shi published the artcileDesign, synthesis and biological evaluation of bicyclic carboxylic acid derivatives as IDO1 inhibitors, Application In Synthesis of 104-01-8, the main research area is immunotherapy tryptophan IDO1 inhibitors Hela cell assay; Hela cell assay; IDO1 inhibitors; Immunotheraphy; l-tryptophan.

Indoleamine 2,3-dioxygenase 1 (IDO1) plays a vital role in tumor immune escape and has emerged as a promising target for cancer immunotherapy. In this study, a novel series of bicyclic carboxylic acid derivatives were designed, synthesized and evaluated for inhibitory activities against IDO1. Among these, compound 9c exhibited strong IDO1 inhibitory activity (HeLa cellular IC50 = 2.6 nM, THP-1 cellular IC50 = 11.2 nM). Further anti-tumor studies in vivo have shown that compound 9c has a great inhibitory effect on tumor growth in mice CT26 model as a single agent or in combination with 5-fluorouracil (inhibition rate was 53.9% and 92.7%, resp.). These results indicate that compound 9c is a effective IDO1 inhibitor for further investigation.

Bioorganic 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, Application In Synthesis of 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Leung, Euphemia published the artcileThe cytotoxic potential of cationic triangulenes against tumor cells, Recommanded Product: 1,3-Dimethoxybenzene, the main research area is cytotoxic potential cationic triangulene tumor cell.

TOTA (trioxatriangulenium ion) is a close-shelled carbocation known to intercalate strongly with the DNA double helix. The cytotoxicity of TOTA and its four close structural analogs, ADOTA, Pr-ADOTA, Pr-DAOTA and n-Butyl-TATA were tested against the breast cancer cell line MDA-MB-231 and colon cancer cell line HCT116. The most potent derivatives Pr-ADOTA and Pr-DAOTA had IC50 values of ∼80 nM for MDA-MB-231 but slightly higher for HCT116 in the low hundreds nM range. A 3D model assay of HCT116 spheroids was also used, mimicking a tumor environment, again both Pr-ADOTA and Pr-DAOTA were very active with IC50 values of 38 nM and 21 nM, resp. Mol. modeling suggest that the planar derivatives intercalate between the base pairs of the DNA double helix. However, only modest DNA double stranded DNA cleavage was observed using the γH2AX assay as compared to camptothecin, a topoisomerase I poison suggesting a different mechanism. Finally, a robust d. functional theory (DFT) model was built to predict the pKR+ stability values, i.e., to design derivatives, which predominantly have a non-intercalating buckled form in healthy tissues followed by a nucleophilic attach of water on the central carbon, but a planar form at relatively low pH values rendering them only cytotoxic in the interior of tumors.

MedChemComm published new progress about Antitumor agents. 151-10-0 belongs to class isoquinoline, name is 1,3-Dimethoxybenzene, and the molecular formula is C8H10O2, Recommanded Product: 1,3-Dimethoxybenzene.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Li, Guangzhe published the artcileTotal synthesis and biological evaluation of 7-hydroxyneolamellarin A as hypoxia-inducible factor-1α inhibitor for cancer therapy, Application of 4-Methoxyphenylacetic acid, the main research area is hydroxyneolamellarin antitumor agent HIF alpha inhibitor; 7-Hydroxyneolamellarin A; Anti-tumor; HIF-1α inhibition; Total synthesis.

7-Hydroxyneolamellarin A (7-OH-Neo A, 1), a natural marine product derived from sponge Dendrilla nigra, was first synthesized with 10% overall yield under the instruction of convergent synthetic strategy. We found that 7-Hydroxyneolamellarin A could attenuate the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibit vascular epidermal growth factor (VEGF) transcriptional activity, showing well inhibitory effect on HIF-1 signaling pathway. Meantime, 7-Hydroxyneolamellarin A had the well anti-tumor activities, such as inhibiting tumor angiogenesis, proliferation, migration and invasion. More importantly, 7-Hydroxyneolamellarin A exhibited profound anti-tumor effect in mice breast cancer model by suppressing the accumulation of HIF-1α in tumor tissue. Mechanism study demonstrated that 7-Hydroxyneolamellarin A might target the protein with the ability of stabilizing HIF-1α in hypoxia. Due to the excellent water solubility, superior anti-tumor activity and good biocompatibility, 7-OH-Neo A shows the promising potential for being exploited as an anti-tumor agent in near future.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Application of 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Yamani, Abdellah published the artcileDiscovery and optimization of novel pyrazole-benzimidazole CPL304110 as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3), Application In Synthesis of 151-10-0, the main research area is pyrazolyl benzimidazole preparation antitumor docking FGFR inhibitor; Anti-tumor activity; FGFR (1–3) inhibitor; Pyrazole-benzimidazole.

The scaffolds hybridization approach, scaffold-hopping concept, has been employed to synthesize a series of novel pyrazole-benzimidazoles I [R1 = H, Cl; R2 = morpholin-4-yl, 4-methylpiperazin-1-ylcarbonyl, tetrahydropyran-4-ylcarbamoyl, etc.; R3 = H, F]. Compound I [R1 = R3 = H; R2 = 4-methylpiperazin-1-yl] (CPL304110) was identified as a selective and potent pan-FGFR inhibitor for FGFR1, FGFR2, FGFR3 with IC50 of 0.75 nM, 0.50 nM, 3.05 nM resp., and IC50 of 87.90 nM for FGFR4. Due to its favorable pharmacokinetic profile, low toxicity and potent anti-tumor activity in-vivo, this compound I is currently under evaluation in phase I clin. trial for the treatment of bladder, gastric and squamous cell lung cancers (01FGFR2018; NCT04149691).

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 151-10-0 belongs to class isoquinoline, name is 1,3-Dimethoxybenzene, and the molecular formula is C8H10O2, Application In Synthesis of 151-10-0.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Maadwar, Sasikala published the artcileA facile and an efficient synthesis of 3, 3-disubstituted oxindole scaffolds and their cytotoxic properties, Category: isoquinoline, the main research area is diphenyl indolinone preparation antitumor activity SAR.

3,3-Disubstituted oxindole derivatives I [R = H, Me, Cl, etc.; R1 = 1,2-dimethoxy, 1,3-dimethoxy, 1,4-dimethoxy, 1,3,5-trimethoxy] were synthesized by treating isatins with electron rich benzene derivatives at room temperature by using BF3·O(Et)2 as catalyst which reduced the synthesis time. The compounds I were evaluated for cytotoxic activity against human breast cancer cells (MCF7) and human ovarian carcinoma cells (SKVO3) by using MTT assay. Compounds I [R = Cl, Br; R1 = 1,3,5-trimethoxy] (7.2±0.22μM and 11.80.21±μM), 2(7.10.24±μM and 9.8±0.27μM), exhibited relatively higher cytotoxic activity against both MCF7 and SKVO3 cell lines, resp.

International Research Journal of Pharmacy published new progress about Antitumor agents. 151-10-0 belongs to class isoquinoline, name is 1,3-Dimethoxybenzene, and the molecular formula is C8H10O2, Category: isoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem