Day: October 17, 2022

Hu, Yijie; Ye, Liufeiyang; Chen, Jie; Zhang, Hui; Deng, Hongmei; Lin, Jin-Hong; Cao, Weiguo published the artcile< An Efficient Construction of CF3-Substituted Spirooxindole-Fused Benzo[a]quinolizidines by a Three-Component Cyclization>, Recommanded Product: 5-Methoxyisoquinoline, the main research area is isoquinoline perfluoroalkylpropiolate oxoindolinylidene propanedinitrile three component cyclization; perfluoroalkyl dicyano spirooxindoline benzoquinolizidine carboxylate preparation.

A convenient three-component cyclization was described for the efficient construction of CF3-substituted spirooxindole-fused benzo[a]quinolizidines by using CF3-propiolate as a building block. This attractive protocol may find great synthetic utility since CF3-containing complex structures were installed by a one-step cyclization under mild conditions.

European Journal of Organic Chemistry published new progress about Alkynes, fluoro Role: RCT (Reactant), RACT (Reactant or Reagent). 90806-58-9 belongs to class isoquinoline, and the molecular formula is C10H9NO, Recommanded Product: 5-Methoxyisoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Pumuye, Paul P.; Evison, Benny J.; Konda, Shyam K.; Collins, J. Grant; Kelso, Celine; Medan, Jelena; Sleebs, Brad E.; Watson, Keith; Phillips, Don R.; Cutts, Suzanne M. published the artcile< Formaldehyde-activated WEHI-150 induces DNA interstrand crosslinks with unique structural features>, Computed Properties of 144511-13-7, the main research area is formaldehyde WEHI150 DNA interstrand crosslink; Anthracenediones; Cancer chemotherapy; DNA sequence specificity; Drug-DNA adducts; Mitoxantrone analogues.

Mitoxantrone is an anticancer anthracenedione that can be activated by formaldehyde to generate covalent drug-DNA adducts. Despite their covalent nature, these DNA lesions are relatively labile. It was recently established that analogs of mitoxantrone featuring extended side-chains terminating in primary amino groups typically yielded high levels of stable DNA adducts following their activation by formaldehyde. In this study we describe the DNA sequence-specific binding properties of the mitoxantrone analog WEHI-150 which is the first anthracenedione to form apparent DNA crosslinks mediated by formaldehyde. The utility of this compound lies in the versatility of the covalent binding modes displayed. Unlike other anthracenediones described to date, WEHI-150 can mediate covalent adducts that are independent of interactions with the N-2 of guanine and is capable of adduct formation at novel DNA sequences. Moreover, these covalent adducts incorporate more than one formaldehyde-mediated bond with DNA, thus facilitating the formation of highly lethal DNA crosslinks. The versatility of binding observed is anticipated to allow the next generation of anthracenediones to interact with a broader spectrum of nucleic acid species than previously demonstrated by the parent compounds, thus allowing for more diverse biol. activities.

Bioorganic & Medicinal Chemistry published new progress about Crosslinking agents. 144511-13-7 belongs to class isoquinoline, and the molecular formula is C13H5F2NO2, Computed Properties of 144511-13-7.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Cheng, Yunfeng; Ni, Nanting; Yang, Wenqian; Wang, Binghe published the artcile< A New Class of Fluorescent Boronic Acids That Have Extraordinarily High Affinities for Diols in Aqueous Solution at Physiological pH>, Application of C9H8BNO2, the main research area is fluorescent boronate high affinity diol aqueous solution physiol pH.

The boronic acid group is an important recognition moiety for sensor design. Herein, the authors report a series of isoquinolinylboronic acids that have extraordinarily high affinities for diol-containing compounds at physiol. pH. In addition, 5- and 8-isoquinolinylboronic acids also showed fairly high binding affinities towards D-glucose (Ka=42 and 46 M-1, resp.). For the first time, weak but encouraging binding of cis-cyclohexanediol was found for these boronic acids. Such binding was coupled with significant fluorescence changes. Furthermore, 4- and 6-isoquinolinylboronic acids also showed the ability to complex Me α-D-glucopyranose (Ka=3 and 2 M-1, resp.).

Chemistry – A European Journal published new progress about Affinity. 721401-43-0 belongs to class isoquinoline, and the molecular formula is C9H8BNO2, Application of C9H8BNO2.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Liao, Lan-Shan; Tan, Lin-Jie; Chen, Yin; Yang, Qi-Yuan; Choudhary, Muhammad Iqbal; Pan, Ying-Ming; Tang, Hai-Tao; Su, Gui-Fa; Liang, Hong; Chen, Zhen-Feng published the artcile< One-pot synthesis of oxoaporphines as potent antitumor agents and investigation of their mechanisms of actions>, Reference of 721401-43-0, the main research area is oxoporphine derivative preparation antitumor agents; Antitumor activity; Apoptosis; Cell cycle; Oxoaporphine.

An efficient one-pot reaction for the synthesis of oxoaporphine alkaloids has been developed. Twenty-three compounds of oxoaporphine alkaloids were prepared and assessed for their antitumor activities. Most compounds inhibited the growth of T-24 tumor cells in vitro. Particularly, I displayed the most potent activity with an IC50 value of 0.5μM, which was 19-fold more potent than the parent compound 4. The substitution at C3-position of oxoaporphine core by -NO2 significantly enhanced the anticancer activity. Mechanism studies indicated that II and I induced cell cycle arrest at G2/M phase; in contrast, III induced cell cycle arrest at the S phase. Increase of mitochondrial ROS/Ca2+ and decrease of MMP, accompanied by activation of caspase-3/9, were observed in T-24 cells after exposure to compounds I, II and III, suggesting that the mitochondrial pathway was involved in the induced apoptosis. Moreover, compound I effectively inhibited tumor growth in a mouse xenograft model bearing T-24.

European Journal of Medicinal Chemistry published new progress about Alkaloids Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), BIOL (Biological Study), PREP (Preparation). 721401-43-0 belongs to class isoquinoline, and the molecular formula is C9H8BNO2, Reference of 721401-43-0.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem