A Structured–Activity Relationship Study of Batracylin Analogues

Yilin Luo; Yun Feng Ren; Ting Chao Chou; Allan Y. Chen; Chiang Yu; Leroy F. Liu; C. C. Cheng

doi:10.1023/A:1018929815422

A Structured–Activity Relationship Study of Batracylin Analogues

Yilin Luo, Yun Feng Ren, Ting Chao Chou, Allan Y. Chen, Chiang Yu, Leroy F. Liu, C. C. Cheng

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

29 Citations (Scopus)

Abstract

A number of isoindolo[l ,2- b]quinazolines and some benzo[4,5]isoquinolino[l,2- b]quinazolines as structural modification analogues of the antitumor compound batracylin were synthesized and evaluated against HL-60 cell growth and in topoisomerase II-mediated DNA cleavage assays. Of the compounds studied, 10,12-dihydro-7,8-methy lenedioxyisoindolo[ 1,2- b] quinazolin-12(10 H)-one 1d, 2-amino-10,12-dihydroisoindolo[l ,2- b]quinazolin- 12(10 H)-one 1p, and 2-amino-7,8-methylenedioxy-10,12-dihydroisoindolo[l ,2- b]quinazolin-12(10 H)-one 1ab exhibited good inhibitory activities against HL-60 cell lines as well as induction of topo II-mediated DNA cleavage activities.

Original language	English
Pages (from-to)	918-923
Number of pages	6
Journal	Pharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists
Volume	10
Issue number	6
DOIs	https://doi.org/10.1023/A:1018929815422
Publication status	Published - Jun 1993
Externally published	Yes

Keywords

DNA topoisomerase
colon adenocarcinoma 38
cytotoxicity
isoindolo[l,2- b]quinazolines
structure–activity relationship

ASJC Scopus subject areas

Pharmacology (medical)
Molecular Medicine
Biotechnology
Pharmacology
Pharmaceutical Science
Organic Chemistry

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10.1023/A:1018929815422

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title = "A Structured–Activity Relationship Study of Batracylin Analogues",

abstract = "A number of isoindolo[l ,2- b]quinazolines and some benzo[4,5]isoquinolino[l,2- b]quinazolines as structural modification analogues of the antitumor compound batracylin were synthesized and evaluated against HL-60 cell growth and in topoisomerase II-mediated DNA cleavage assays. Of the compounds studied, 10,12-dihydro-7,8-methy lenedioxyisoindolo[ 1,2- b] quinazolin-12(10 H)-one 1d, 2-amino-10,12-dihydroisoindolo[l ,2- b]quinazolin- 12(10 H)-one 1p, and 2-amino-7,8-methylenedioxy-10,12-dihydroisoindolo[l ,2- b]quinazolin-12(10 H)-one 1ab exhibited good inhibitory activities against HL-60 cell lines as well as induction of topo II-mediated DNA cleavage activities.",

keywords = "DNA topoisomerase, colon adenocarcinoma 38, cytotoxicity, isoindolo[l,2- b]quinazolines, structure–activity relationship",

author = "Yilin Luo and Ren, {Yun Feng} and Chou, {Ting Chao} and Chen, {Allan Y.} and Chiang Yu and Liu, {Leroy F.} and Cheng, {C. C.}",

year = "1993",

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AU - Luo, Yilin

AU - Ren, Yun Feng

AU - Chou, Ting Chao

AU - Chen, Allan Y.

AU - Yu, Chiang

AU - Liu, Leroy F.

AU - Cheng, C. C.

PY - 1993/6

Y1 - 1993/6

N2 - A number of isoindolo[l ,2- b]quinazolines and some benzo[4,5]isoquinolino[l,2- b]quinazolines as structural modification analogues of the antitumor compound batracylin were synthesized and evaluated against HL-60 cell growth and in topoisomerase II-mediated DNA cleavage assays. Of the compounds studied, 10,12-dihydro-7,8-methy lenedioxyisoindolo[ 1,2- b] quinazolin-12(10 H)-one 1d, 2-amino-10,12-dihydroisoindolo[l ,2- b]quinazolin- 12(10 H)-one 1p, and 2-amino-7,8-methylenedioxy-10,12-dihydroisoindolo[l ,2- b]quinazolin-12(10 H)-one 1ab exhibited good inhibitory activities against HL-60 cell lines as well as induction of topo II-mediated DNA cleavage activities.

AB - A number of isoindolo[l ,2- b]quinazolines and some benzo[4,5]isoquinolino[l,2- b]quinazolines as structural modification analogues of the antitumor compound batracylin were synthesized and evaluated against HL-60 cell growth and in topoisomerase II-mediated DNA cleavage assays. Of the compounds studied, 10,12-dihydro-7,8-methy lenedioxyisoindolo[ 1,2- b] quinazolin-12(10 H)-one 1d, 2-amino-10,12-dihydroisoindolo[l ,2- b]quinazolin- 12(10 H)-one 1p, and 2-amino-7,8-methylenedioxy-10,12-dihydroisoindolo[l ,2- b]quinazolin-12(10 H)-one 1ab exhibited good inhibitory activities against HL-60 cell lines as well as induction of topo II-mediated DNA cleavage activities.

KW - DNA topoisomerase

KW - colon adenocarcinoma 38

KW - cytotoxicity

KW - isoindolo[l,2- b]quinazolines

KW - structure–activity relationship

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A Structured–Activity Relationship Study of Batracylin Analogues

Abstract

Keywords

ASJC Scopus subject areas

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