Antitumor agents—CLXXIII. Synthesis and evaluation of camptothecin-4β-amino-4′-O-demethyl epipodophyllotoxin conjugates as inhibitors of mammalian DNA …

KF Bastow, HK Wang, YC Cheng, KH Lee - Bioorganic & Medicinal …, 1997 - Elsevier
Two conjugates composed of a camptothecin and a 4′-O-demethyl epipodophyllotoxin
derivative joined by an imine linkage were prepared and evaluated as inhibitors of …

Structural basis for topoisomerase I inhibition by nucleoside analogs

WH Gmeiner, S Yu, RT Pon, P Pourquier… - … and Nucleic Acids, 2003 - Taylor & Francis
Nucleoside analogs such as 1-β-D-arabinofuranosyl cytidine (AraC) and 2′, 2′-difluoro
deoxycytidine (dFdC) are important components of the anticancer chemotherapeutic arsenal …

Molecular modeling studies of the DNA− topoisomerase I ternary cleavable complex with camptothecin

Y Fan, JN Weinstein, KW Kohn, LM Shi… - Journal of medicinal …, 1998 - ACS Publications
The present studies provide a three-dimensional model for the postulated ternary cleavable
complex of topoisomerase I (top1), DNA, and camptothecin (CPT). Molecular simulations …

Position-specific trapping of topoisomerase I–DNA cleavage complexes by intercalated benzo[a]- pyrene diol epoxide adducts at the 6-amino group of adenine

Y Pommier, GS Laco, G Kohlhagen… - Proceedings of the …, 2000 - National Acad Sciences
DNA topoisomerase I (top1) is the target of potent anticancer agents, including
camptothecins and DNA intercalators, which reversibly stabilize (trap) top1 catalytic …

The synthesis of 5-substituted camptothecins as potential inhibitors of DNA topoisomerase I

HK Wang, SY Lin, KM Hwang, AT McPhail… - Bioorganic & Medicinal …, 1995 - Elsevier
Four new 5-substituted camptothecins (4–7) have been synthesized and evaluated for DNA
topoisomerase I inhibition. The results suggested that the pyridone moiety in the D ring of …

Synthesis of novel water-soluble 7-(aminoacylhydrazono)-formyl camptothecins with potent inhibition of DNA topoisomerase I

HK Wang, SY Liu, KM Hwang, G Taylor… - Bioorganic & medicinal …, 1994 - Elsevier
Abstract Eighteen new water-soluble 7-(aminoacylhydrazono)-formyl camptothecins were
synthesized and evaluated for their ability to cause protein-linked DNA breaks and to inhibit …

Human topoisomerase I inhibition: docking camptothecin and derivatives into a structure-based active site model

GS Laco, JR Collins, BT Luke, H Kroth, JM Sayer… - Biochemistry, 2002 - ACS Publications
Human topoisomerase I (top1) is an important target for anti-cancer drugs, which include
camptothecin (CPT) and its derivatives. To elucidate top1 inhibition in vitro, we made a …

Synthesis of new camptothecin analogs with improved antitumor activities

S Niizuma, M Tsukazaki, H Suda, T Murata… - Bioorganic & medicinal …, 2009 - Elsevier
Novel hexacyclic camptothecin analogs containing cyclic amidine, urea, or thiourea moiety
were designed and synthesized based on the proposed 3D-structure of the topoisomerase I …

Recognition and cleavage of DNA by rebeccamycin-or benzopyridoquinoxaline conjugated of triple helix-forming oligonucleotides

PB Arimondo, P Moreau, A Boutorine, C Bailly… - Bioorganic & medicinal …, 2000 - Elsevier
Indolocarbazole and benzopyridoquinoxaline derivatives have been shown to have anti-
tumor activity and to stimulate DNA topoisomerase I-mediated cleavage. Two …

Novel 7-alkyl methylenedioxy-camptothecin derivatives exhibit increased cytotoxicity and induce persistent cleavable complexes both with purified mammalian …

M Valenti, W Nieves-Neira, G Kohlhagen… - Molecular …, 1997 - ASPET
An alkylating camptothecin (CPT) derivative, 7-chloromethyl-10, 11-methylenedioxy-
camptothecin (7-CM-MDO-CPT) was recently shown to produce irreversible topoisomerase I …