Record Details

QUINAZOLINE CLUBBED s-TRIAZINE DERIVATIVES AS KINASE INHIBITOR: DESIGN, SYNTHESIS AND ANTICANCER ACTIVITY

KrishiKosh

View Archive Info
 
 
Field Value
 
Title QUINAZOLINE CLUBBED s-TRIAZINE DERIVATIVES AS KINASE INHIBITOR: DESIGN, SYNTHESIS AND ANTICANCER ACTIVITY
 
Creator PATHAK, PRATEEK
 
Contributor Verma, Prof. (Dr.) Amita
Kumar, Dr. Vikas
 
Subject null
 
Description Three different congeneric series of quinazoline derivatives were synthesized via multi steps
reaction and evaluated for their in-vitro anticancer activity and further in-ovo antiangiogenic
activity using cancer induced chick egg against HeLa (Human cervical cancer), MCF-7
(Human breast cancer cell), HL-60 (Human promyelocytic leukemia cell) and HepG2
(Human Hepatocellular carcinoma cell) and TPC-1 (Thyroid cancer cell) respectively during
both assays. Derivatives 12d, 12j, 12k found significantly active against HeLa cell line,
derivatives 13f, 14f, 14h, 14k, 14l, 14m showed significant potency against TPC-1 cell line,
derivatives 12b, 12l, 13m against HeLa and MCF-7 cell lines both during MTT assay.
Whereas, cancer induced CAM assay stated that derivatives 12l, 12m, 12d were potent
against HeLa and MCF-7 cell lines, derivatives 12g, 14b, 14k were significant active against
MCF-7 cell line. Apart from these derivatives 12j against HeLa, derivative, derivative 13d
against TPC-1 and MCF-7, derivatives 14a, 14e, 14i, 14j, and 14l against TPC-1 were
significantly potent. The observed activity was further substantiated by docking study on
VGFR2 and FAK. On the basis of SAR, it may be concluded that the potency of drugs
depends on the nature of aliphatic substitution and the heterocyclic ring system.
 
Date 2018-04-13T05:00:32Z
2018-04-13T05:00:32Z
2017
 
Type Thesis
 
Identifier http://krishikosh.egranth.ac.in/handle/1/5810043383
 
Language en
 
Format application/pdf
 
Publisher DEPARTMENT OF PHARMACEUTICAL SCIENCES FACULTY OF HEALTH SCIENCES SAM HIGGINBOTTOM UNIVERSITY OF AGRICULTURE, TECHNOLOGY AND SCIENCES ALLAHABAD (U.P.) INDIA