Synthesis, antitumor evaluation, and molecular docking studies of indole-indazolyl hydrazide-hydrazone derivatives

被引：44

作者：

Sreenivasulu, Reddymasu ^{[1
]}

Sujitha, Pombala ^{[4
]}

Jadav, Surender Singh ^{[2
]}

Ahsan, Mohamed Jawed ^{[3
]}

Kumar, C. Ganesh ^{[4
]}

Raju, Rudraraju Ramesh ^{[1
]}

机构：

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

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

[3] Maharishi Arvind Coll Pharm, Dept Pharmaceut Chem, Jaipur 302023, Rajasthan, India

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

来源：

MONATSHEFTE FUR CHEMIE | 2017年 / 148卷 / 02期

关键词：

Indole; Indazole; Breast cancer; Tubulin; Docking; BREAST-CANCER CELLS; ANTIPROLIFERATIVE ACTIVITY; BENZYLIDENE-HYDRAZIDES; EFFICIENT SYNTHESIS; ANTICANCER ACTIVITY; CYTOTOXIC AGENTS; POTENT; INHIBITORS; 2-PHENYLINDOLE-3-CARBALDEHYDES; ANTAGONISTS;

D O I：

10.1007/s00706-016-1750-6

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of ten novel hydrazide-hydrazones linked indole and indazole moieties were designed and synthesized. All the synthesized compounds were evaluated for their cytotoxicity against four human cancer cell lines (HeLa, MDA-MB-231, MCF-7, and A549). Three of the synthesized compounds showed promising cytotoxicity specifically on some of the tested cell lines with IC50 values ranging between 1.93 and 25.6 mu M. Further, one compound was identified as a promising drug lead which showed promising cytotoxicity with IC50 value of 1.93 mu M towards MCF-7 breast cancer cell line as compared to the standard drug doxorubicin (IC50 value 0.98 mu M). While, all these new compounds showed no cytotoxicity on the normal human embryonic kidney cell line, HEK-293.

引用

页码：305 / 314

页数：10

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