Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents

Mohd Rashid; Asif Husain; Mohammad Shaharyar; Ravinesh Mishra; Afzal Hussain; Obaid Afzal

doi:10.1016/j.ejmech.2014.06.033

Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents

Mohd Rashid, Asif Husain, Mohammad Shaharyar, Ravinesh Mishra, Afzal Hussain, Obaid Afzal

Jamia Hamdard University

Research output: Contribution to journal › Article › peer-review

37 Scopus citations

Abstract

Design and synthesis of new pyrimidine derivatives clubbed with thiazolidin-4-one from 4-(2-chlorophenyl)-6-(2,4-dichlorophenyl)pyrimidin-2- amine and their in vitro anticancer activities were screened at National Cancer Institute (NCI), USA against full NCI 60 cell lines. Compound 2 (NSC: 765735) exhibited remarkable growth inhibition at single dose (10 μM) and encourage chosen for broadcast at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM). The compound 2 was found better quality for Lung cancer cell line (HOP-92) by viewing growth inhibition (GI₅₀ 0.52) and no cytotoxicity seen (LC₅₀ > 100). Molecular docking study was performed using Maestro 9.0 (Schrodinger Inc. USA) to provide binding mode into binding sites of CDK2. Compound 2 could be used as a lead compound for developing new potential anticancer agents.

Original language	English
Pages (from-to)	630-645
Number of pages	16
Journal	European Journal of Medicinal Chemistry
Volume	83
DOIs	https://doi.org/10.1016/j.ejmech.2014.06.033
State	Published - 18 Aug 2014
Externally published	Yes

Keywords

CDK 2 enzyme
In-vitro anticancer activity
NCI 60 cell line
Thiazolidin-4-one

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1016/j.ejmech.2014.06.033

Cite this

@article{e797fc80223d4e3b94659d6db40a4906,

title = "Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents",

abstract = "Design and synthesis of new pyrimidine derivatives clubbed with thiazolidin-4-one from 4-(2-chlorophenyl)-6-(2,4-dichlorophenyl)pyrimidin-2- amine and their in vitro anticancer activities were screened at National Cancer Institute (NCI), USA against full NCI 60 cell lines. Compound 2 (NSC: 765735) exhibited remarkable growth inhibition at single dose (10 μM) and encourage chosen for broadcast at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM). The compound 2 was found better quality for Lung cancer cell line (HOP-92) by viewing growth inhibition (GI50 0.52) and no cytotoxicity seen (LC50 > 100). Molecular docking study was performed using Maestro 9.0 (Schrodinger Inc. USA) to provide binding mode into binding sites of CDK2. Compound 2 could be used as a lead compound for developing new potential anticancer agents.",

keywords = "CDK 2 enzyme, In-vitro anticancer activity, NCI 60 cell line, Thiazolidin-4-one",

author = "Mohd Rashid and Asif Husain and Mohammad Shaharyar and Ravinesh Mishra and Afzal Hussain and Obaid Afzal",

year = "2014",

month = aug,

day = "18",

doi = "10.1016/j.ejmech.2014.06.033",

language = "English",

volume = "83",

pages = "630--645",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

}

TY - JOUR

T1 - Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents

AU - Rashid, Mohd

AU - Husain, Asif

AU - Shaharyar, Mohammad

AU - Mishra, Ravinesh

AU - Hussain, Afzal

AU - Afzal, Obaid

PY - 2014/8/18

Y1 - 2014/8/18

N2 - Design and synthesis of new pyrimidine derivatives clubbed with thiazolidin-4-one from 4-(2-chlorophenyl)-6-(2,4-dichlorophenyl)pyrimidin-2- amine and their in vitro anticancer activities were screened at National Cancer Institute (NCI), USA against full NCI 60 cell lines. Compound 2 (NSC: 765735) exhibited remarkable growth inhibition at single dose (10 μM) and encourage chosen for broadcast at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM). The compound 2 was found better quality for Lung cancer cell line (HOP-92) by viewing growth inhibition (GI50 0.52) and no cytotoxicity seen (LC50 > 100). Molecular docking study was performed using Maestro 9.0 (Schrodinger Inc. USA) to provide binding mode into binding sites of CDK2. Compound 2 could be used as a lead compound for developing new potential anticancer agents.

AB - Design and synthesis of new pyrimidine derivatives clubbed with thiazolidin-4-one from 4-(2-chlorophenyl)-6-(2,4-dichlorophenyl)pyrimidin-2- amine and their in vitro anticancer activities were screened at National Cancer Institute (NCI), USA against full NCI 60 cell lines. Compound 2 (NSC: 765735) exhibited remarkable growth inhibition at single dose (10 μM) and encourage chosen for broadcast at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM). The compound 2 was found better quality for Lung cancer cell line (HOP-92) by viewing growth inhibition (GI50 0.52) and no cytotoxicity seen (LC50 > 100). Molecular docking study was performed using Maestro 9.0 (Schrodinger Inc. USA) to provide binding mode into binding sites of CDK2. Compound 2 could be used as a lead compound for developing new potential anticancer agents.

KW - CDK 2 enzyme

KW - In-vitro anticancer activity

KW - NCI 60 cell line

KW - Thiazolidin-4-one

UR - http://www.scopus.com/inward/record.url?scp=84903946751&partnerID=8YFLogxK

U2 - 10.1016/j.ejmech.2014.06.033

DO - 10.1016/j.ejmech.2014.06.033

M3 - Article

C2 - 25010935

AN - SCOPUS:84903946751

SN - 0223-5234

VL - 83

SP - 630

EP - 645

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents

Abstract

Keywords

UN SDGs

Access to Document

Other files and links

Fingerprint

Cite this