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 › peer-review

51 Scopus citations

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
State	Published - Mar 10 2011
Externally published	Yes

Keywords

5:7:5-fused tricycles
Synthesis
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

UN SDGs

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

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10.1021/ml100281b

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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, Synthesis, 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",

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",

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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 - Synthesis

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

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DO - 10.1021/ml100281b

M3 - Article

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JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

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ER -

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

Abstract

Keywords

UN SDGs

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