Structure-Activity Relationships of Anti-Tumour Agents
The Workshop series of the "Koningin Wilhelmina Fonds" is a feature of the interest of this Foundation to promote research and education in the field of cancer, aiming to improve prognosis of the cancer patient. For almost a century, surgery has now been
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DEVELOPMENTS IN PHARMACOLOGY VOLUME 3
1. J.M. Boeynaems and A.G. Herman, eds.: Prostaglandins, prostacyclin, and thromboxanes measurement. 1980. ISBN 90 247 2417 1. 2. R.M. Berne, Th.W. Rail and R. Rubio, eds.: Regulatory function in adenosine. 1983. ISBN 902472779 O.
STRUCTURE -ACTIVITY RELATIONSHIPS OF ANTI-TUMOUR AGENTS Edited by
D.N. Reinhoudt
Department of Organic Chemistry Technical University Twente, Enschede, The Netherlands
T .A. Connors
MRC Toxicology Unit Medical Research Council Laboratories Carshalton, Surrey, Great Britain
H.M. Pinedo
Department of Biochemistry Antonie van Leeuwenhoekziekenhu is Amsterdam, The Netherlands
K.W. van de Poll
Koningin Wilhelmina Fonds The Netherlands Cancer Foundation Amsterdam, The Netherlands
1983
MARTINUS NIJHOFF PUBLISHERS THE HAGUE / BOSTON / LONDON
Distributors: for the United States and Canada Kluwer Boston, Inc. 190 Old Derby Street Hingham. MA 02043 USA jf" all other co un tries
Kluwer Academic Publishers Group Distribution Center P.O. Box 322 3300 AH Dordrecht The Netherlands
Librar.\" of Congress Cataloging in Publi(,~tion Data
Main
ent~y
under title:
Structure-activity relationships of anti-tumour agp.nts.
(Developments in pharmacology; v. 3) Papers presented at a workshop held Mar. 11-13, 1982. 1. Cancer--Chemotherapy--Congresses. 2. Antineoplastic agents--Congresses. 3. Structure-activity relationship (Pharmacology)--Congresses. 1. Reinhoudt, D. N. II. Series. [DNLM: 1. Structure -activity relationship--Congresses. 2. Antineoplastic agents--Congresses. WI DE998NK v. 3 I QV 269J
RC271.C5S77
1983
616.99'4061
ISBN-13:978-94-009-6800-4 001: 10.1007/978-94-009-6798-4
82-19101
e-ISBN-13:978-94-009-6798-4
Copyright C!.\ 1983 by Martinus Nijhoff Publishers, The Hague, Boston, London. Softcover reprint of the hardcover 1st edition 1983
All rights reserved. No part of this publication may be reproduced, stored in a retrieval system, or transmilled in an~' form or by any means, mechanical, photocopying, recording, or otherwise, without the prior written permission of the publisher, Martinus NijhofIPublishers. P.O. Box 566, 2501 eN The Hague, The Netherlands.
CONTENTS
LIST OF AUTHORS - PARTICIPANTS
VII
1. INTRODUCTION H.M. Pinedo 2. STRATEGY FOR THE DISCOVERY AND DEVELOPMENT OF NOVEL ANTICANCER AGENTS V.L. Narayanan
5
3. QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP STUDIES AROUND CYTOTOXIC DRUGS R.F. Rekker
23
4. ALKYLATING PRODRUGS IN CANCER CHEMOTHERAPY T.A. Connors
47
5. STRUCTURE-ACTIVITY RELATIONSHIPS FOR ANTI-TUMOUR PLATINUM COMPLEXES M.J. Cleare
59
6. BIOREDUCTIVE ALKYLATION - NATURALLY OCCURRING QUINONES AS POTENTIAL CANDIDATES H.W. Moore, K.F. West, K. Srinivasacher and R. Czerniak
93
7. STRUCTURE-ACTIVITY RELATIONSHIPS IN DOXOn.uBICIN RELATED COl1POUNDS F. Arcamone
111
8. STRUCTURE-ACTIVITY RELATIONSHIPS AMONG ANTITUMOUR QUINONES J.S. Driscoll
135
9. IN OF B. S.
149
VITRO OXIDATIVE ACTIVATION: A MODEL FOR THE CYTOTOXIC ACTION 9-HYDROXY ELLIPTICINE DERIVATIVES Meunier, C. Auclair, J. Bernadou, G. Meunier, M. M
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