Synthesis, anticancer evaluation and molecular docking studies of bis(indolyl) triazinones, Nortopsentin analogs

被引：36

作者：

Sreenivasulu, Reddymasu ^{[1
]}

Durgesh, Rudavath ^{[1
]}

Jadav, Surender Singh ^{[2
]}

Sujitha, Pombala ^{[3
]}

Kumar, C. Ganesh ^{[3
]}

Raju, Rudraraju Ramesh ^{[1
]}

机构：

[1] Acharya Nagarjuna Univ, Dept Chem, Guntur 522510, Andhra Pradesh, India

[2] Birla Inst Technol, Dept Pharmaceut Sci & Technol, Ranchi 835215, Jharkhand, India

[3] Indian Inst Chem Technol, CSIR, Med Chem & Pharmacol Div, Uppal Rd, Hyderabad 500007, Telangana, India

来源：

CHEMICAL PAPERS | 2018年 / 72卷 / 06期

关键词：

Nortopsentins; Triazinones; Diazo tri keto compounds; Anti-tumor activity; Colchicine; ANTIPROLIFERATIVE ACTIVITY; BIOLOGICAL EVALUATION; ELLIPTICINE DERIVATIVES; BISINDOLE ALKALOIDS; ANTITUMOR-ACTIVITY; NATURAL-PRODUCTS; INDOLE ALKALOIDS; MARINE; INHIBITORS; TOPSENTIN;

D O I：

10.1007/s11696-017-0372-8

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A new series of bis indolyl tri keto diazo compounds and 3,5-bis(3'-indolyl) triazinones were designed and synthesized as anticancer agents. Their anticancer activity was screened in vitro towards four different human cancer cell lines like HeLa, MCF-7, MDA-MB-231 and A549 cell lines. Among them, compounds 17a and 17b showed potent cytotoxicity with inhibition (IC50) values of 4.6 and 1.3 A mu M on Human Cervical cancer cell line, respectively. The in silico simulation studies using ADT 1.5.6 tools revealed unique pi-pi interactions of indole ring of compound 17b with colchicines active site residue Tyr312 could be a valid reason behind its maximum potency when compared to remaining compounds in responsible of its higher activity. [GRAPHICS] .

引用

页码：1369 / 1378

页数：10

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