Novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazodiazepine ring system

Atul Kondaskar; Shilpi Kondaskar; Raj Kumar; James C Fishbein; Nidal Muvarak; Rena G Lapidus; Mariola Sadowska; Martin J Edelman; Guus M Bol; Farhad Vesuna; Venu Raman; Ramachandra S Hosmane

doi:10.1021/ml100281b

Novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazodiazepine ring system

Atul Kondaskar, Shilpi Kondaskar, Raj Kumar, James C Fishbein, Nidal Muvarak, Rena G Lapidus, Mariola Sadowska, Martin J Edelman, Guus M Bol, Farhad Vesuna, Venu Raman, Ramachandra S Hosmane

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

36 Citations (Scopus)

Abstract

Synthesis of a series of novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazo[4,5-d:4′,5′-f][1,3]diazepine ring system is reported. Compounds 1, 2, 8, 11, and 12 in the series show promising in vitro antitumor activity with low micromolar IC₅₀ values against prostate, lung, breast, and ovarian cancer cell lines. Some notions about structure-activity relationships and a possible mechanism of biological activity are presented. Also presented are preliminary in vivo toxicity studies of 1 using SCID mice.

Original language	English
Pages (from-to)	252-256
Number of pages	5
Journal	ACS Medicinal Chemistry Letters
Volume	2
Issue number	3
DOIs	https://doi.org/10.1021/ml100281b
Publication status	Published - 10 Mar 2011
Externally published	Yes

Keywords

5:7:5-fused tricycles
and ovarian cancers
breast
broad spectrum anticancer activity
diimidazo[4,5-d:4′,5′-f][1,3] diazepine ring system
effects on G1 and S phases of the cell cycle
in vitro screening
lung
preliminary mechanistic studies
prostate
Synthesis

Access to Document

10.1021/ml100281b

Cite this

@article{00a90a23a324459bb044469853478fc3,

title = "Novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazodiazepine ring system",

abstract = "Synthesis of a series of novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazo[4,5-d:4′,5′-f][1,3]diazepine ring system is reported. Compounds 1, 2, 8, 11, and 12 in the series show promising in vitro antitumor activity with low micromolar IC50 values against prostate, lung, breast, and ovarian cancer cell lines. Some notions about structure-activity relationships and a possible mechanism of biological activity are presented. Also presented are preliminary in vivo toxicity studies of 1 using SCID mice.",

keywords = "5:7:5-fused tricycles, and ovarian cancers, breast, broad spectrum anticancer activity, diimidazo[4,5-d:4′,5′-f][1,3] diazepine ring system, effects on G1 and S phases of the cell cycle, in vitro screening, lung, preliminary mechanistic studies, prostate, Synthesis",

author = "Atul Kondaskar and Shilpi Kondaskar and Raj Kumar and Fishbein, {James C} and Nidal Muvarak and Lapidus, {Rena G} and Mariola Sadowska and Edelman, {Martin J} and Bol, {Guus M} and Farhad Vesuna and Venu Raman and Hosmane, {Ramachandra S}",

year = "2011",

month = mar,

day = "10",

doi = "10.1021/ml100281b",

language = "English",

volume = "2",

pages = "252--256",

journal = "ACS Medicinal Chemistry Letters",

issn = "1948-5875",

publisher = "American Chemical Society",

number = "3",

}

TY - JOUR

T1 - Novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazodiazepine ring system

AU - Kondaskar, Atul

AU - Kondaskar, Shilpi

AU - Kumar, Raj

AU - Fishbein, James C

AU - Muvarak, Nidal

AU - Lapidus, Rena G

AU - Sadowska, Mariola

AU - Edelman, Martin J

AU - Bol, Guus M

AU - Vesuna, Farhad

AU - Raman, Venu

AU - Hosmane, Ramachandra S

PY - 2011/3/10

Y1 - 2011/3/10

N2 - Synthesis of a series of novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazo[4,5-d:4′,5′-f][1,3]diazepine ring system is reported. Compounds 1, 2, 8, 11, and 12 in the series show promising in vitro antitumor activity with low micromolar IC50 values against prostate, lung, breast, and ovarian cancer cell lines. Some notions about structure-activity relationships and a possible mechanism of biological activity are presented. Also presented are preliminary in vivo toxicity studies of 1 using SCID mice.

AB - Synthesis of a series of novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazo[4,5-d:4′,5′-f][1,3]diazepine ring system is reported. Compounds 1, 2, 8, 11, and 12 in the series show promising in vitro antitumor activity with low micromolar IC50 values against prostate, lung, breast, and ovarian cancer cell lines. Some notions about structure-activity relationships and a possible mechanism of biological activity are presented. Also presented are preliminary in vivo toxicity studies of 1 using SCID mice.

KW - 5:7:5-fused tricycles

KW - and ovarian cancers

KW - breast

KW - broad spectrum anticancer activity

KW - diimidazo[4,5-d:4′,5′-f][1,3] diazepine ring system

KW - effects on G1 and S phases of the cell cycle

KW - in vitro screening

KW - lung

KW - preliminary mechanistic studies

KW - prostate

KW - Synthesis

UR - http://www.scopus.com/inward/record.url?scp=79952649904&partnerID=8YFLogxK

U2 - 10.1021/ml100281b

DO - 10.1021/ml100281b

M3 - Article

C2 - 21572541

SN - 1948-5875

VL - 2

SP - 252

EP - 256

JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

IS - 3

ER -

Novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazodiazepine ring system

Abstract

Keywords

Access to Document

Other files and links

Fingerprint

Cite this