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β- Carbolines
β- Carbolines: A Privileged Scaffold for Modern Drug Discovery provides a summary of methods for the synthesis of various natural products engineered with the diverse
β- carboline scaffold and their biological evaluation.
β- carboline and its derivatives have generated considerable interest in recent years
for their versatile properties in chemistry and pharmacology. This is due to their ability to act as agonists to benzodiazepine receptors, hydroxy serotonin receptors, and intercalate into DNA and to inhibit CDK, topisomerase, and monoamine oxidase enzymes. Their pharmacological properties include anxiolytic, hypnotic, anticonvul­sant, antiviral, antiparasitic, and antimicrobial attributes. This book provides a sum­mary of methods for the synthesis of various natural products engineered with the diverse β- carboline scaffold and their biological evaluation.
Features:
• Focuses on the different application and therapies of β- carbolines.
• Provides a summary of methods for the synthesis of various natural products engineered with the diverse β- carbolines.
• Discusses methods of biological evaluation of β- carbolines.
• Explores different chemical transformations occurring with synthesis using β- carbolines.
• Covers both heterocyclic synthesis and multicomponent synthesis related to β- carboline.
This text is key reading for researchers in medicinal chemistry and drug discovery looking to understand the broad potential of β- carbolines.
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β- Carbolines
A Privileged Scaffold for Modern Drug
Discovery
Edited by
Keshav Lalit Ameta
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Cover illustration: Shutterstock
First edition published 2025 by CRC Press 2385 Executive Center Drive, Suite 320, Boca Raton, FL 33431
and by CRC Press 4 Park Square, Milton Park, Abingdon, Oxon, OX14 4RN
© 2025 Taylor & Francis Group, LLC
CRC Press is an imprint of Taylor & Francis Group, LLC
Reasonable efforts have been made to publish reliable data and information, but the author and publisher cannot assume responsibility for the validity of all materials or the consequences of their use. The authors and publishers have attempted to trace the copyright holders of all material reproduced in this publication and apologize to copyright holders if permission to publish in this form has not been obtained. If any copyright material has not been acknowledged please write and let us know so we may rectify in any future reprint.
Except as permitted under U.S. Copyright Law, no part of this book may be reprinted, reproduced, transmitted, or utilized in any form by any electronic, mechanical, or other means, now known or hereafter invented, including photocopying, microlming, and recording, or in any information storage or retrieval system, without written permission from the publishers.
For permission to photocopy or use material electronically from this work, access www.copyri ght.com or contact the Copyright Clearance Center, Inc. (CCC), 222 Rosewood Drive, Danvers, MA 01923, 978- 750-
8400. For works that are not available on CCC please contact mpkbookspermissions@tandf.co.uk
Trademark notice: Product or corporate names may be trademarks or registered trademarks and are used only for identication and explanation without intent to infringe.
ISBN: 978- 1- 138- 48238- 8 (hbk) ISBN: 978- 1- 032- 41075- 3 (pbk) ISBN: 978- 1- 351- 05803- 2 (ebk)
DOI: 10.1201/ 9781351058032
Typeset in Times by Newgen Publishing UK
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Dedication
To my parents, who gave me the gift of dreams and the
ability to realize them.
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Contents
Foreword ...................................................................................................................ix
Preface .......................................................................................................................xi
About the Editor ......................................................................................................xiii
Contributors .............................................................................................................xv
Chapter 1 β- Carbolines as Anti- Cancer Agents: Synthesis and
Biological Study ................................................................................... 1
Ravikumar M. Borade, Devidas S. Bhagat, Swati B. Kale, Dhanraj P. Kamble, Saroj R. Bembalkar, and Rajendra P. Pawar
Chapter 2 β- Carbolines as Antibacterial Agents: Synthesis and
Biological Study ................................................................................. 52
Shivendra Singh and Shivangi Sharma
Chapter 3 β- Carbolines as Antifungal Agents: Synthesis and
Biological Study ................................................................................. 82
Dattatraya Pansare, Rohini Shelke, Rajita Ingle, Shankar Thopate, Mubarak Shaikh, Aniket Sarkate, and Rajendra P. Pawar
Chapter 4 β- Carbolines as Kinase Inhibitors: Synthesis and
Biological Studies ..............................................................................94
Pankaj Teli, Shivani Soni, Sunita Teli, Dinesh K. Agarwal, Dinesh K. Jangid, and Shikha Agarwal
Chapter 5 Sulfur- containing β- Carbolines: Synthesis and
Biological Study ............................................................................... 126
Vnira R. Akhmetova, Danil V. Leont’ev, and Nail S. Akhmadiev
Chapter 6 Antimalarial Activity and β- Carboline Derivative: A Synthetic
Approach .......................................................................................... 158
Jagannath S. Godse, Santosh B. Gaikwad, Sunil U. Tekale, Sanjay B. Ubale, and Rajendra P. Pawar
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Contents
Chapter 7 β- Carbolines as Antioxidant: Synthesis and Biological Study ......... 179
Chetna Ameta, Monika Kumawat, Dharmendra, and Mukesh Kumar
Chapter 8 β- Carbolines as Anti- inammatory and Antidepressant
Agents: Synthesis and Biological Study ..........................................204
Nidhi Jangir, Surendra Kumar Bagaria, Surbhi Dhadda, Shikha Agarwal, Dinesh Kumar Jangid
Chapter 9 β- Carbolines as Anti- HIV Agents: Synthesis and
Biological Study ............................................................................... 234
Jaymin Parikh, Keyur Bhatt, and Kuldeep V Joshi
Index ...................................................................................................................... 261
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Foreword
In the ever- expanding realm of chemistry of bioactive heterocycles and its applications, the exploration of β- carboline skeleton, representing the basic structural unit of many bioactive heterocycles, stands as a captivating journey into the intricate tapestry of molecular diver­sity. As we embark on this intellectual odyssey through the pages of β- Carboline: A Privileged Scaffold for Modern Drug Discovery, we nd ourselves immersed in a world where bioactive heterocycles create symphonies
of unique biological applications. This edited volume is a testament to the collaborative efforts of brilliant researchers and academicians who have dedicated their time and expertise to unravelling the secrets hidden within β- Carboline moieties.
The chapters within this book are not mere compilations of data or just lists of facts; rather, they are thought- provoking journeys of researchers who understand the complexities of synthesis, characterization, and biological study of differently substituted β- carbolines. From foundational ideas to state- of- the- art developments, the authors have expertly constructed a timeline that pushes the limits of human com­prehension and goes beyond accepted wisdom. I extend my gratitude to the contributors who have shared their intellectual jewels, shaping this book into a treasure trove of knowledge. May the readers nd inspiration within these pages, sparking new ideas and forging ahead on their own quests for understanding.
I cordially welcome you to explore the realm of “β- carbolines” and go beyond conventional knowledge on an engrossing story of molecular discovery, where the indole- pyridine fused framework becomes the main characters. This is all in the spirit of scientic research.
Wishing you a happy reading experience and scientic pursuits as abundant and fullling as the substances found in these pages.
Prof. (Dr.) Rama Shankar Dubey
Vice- Chancellor, Central University of Gujarat, Gandhinagar, Bharat- 382030.
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Preface
Heterocycles offer an extensive variety of structural variations that facilitate the development of varied chemical libraries. The hunt for new medications with enhanced efcacy, fewer side effects, and unique methods of action benets from this diversity. Heterocycles are found in many therapeutic products. To optimize their interactions with target biomolecules, increase bioavailability, and improve pharma­cological characteristics, medicinal chemists often add heterocyclic moieties to drug candidates. Biologically active heterocyclic compounds have been a primary area of interest for organic chemists for many years due to their numerous medicinal prop­erties. In the realm of medicinal chemistry, nitrogen, sulfur, and oxygen- containing ve- and six- membered heterocyclic molecules have held great importance.
β- carbolines are a large group of natural and synthetic indole alkaloids having common tricyclic pyrido[3,4- b]indole ring motif with varying degrees of aromati­city, some of which are widely distributed in nature including various plants, marine creatures, insects, foodstuffs, mammalians as well as human tissues and body uids. This group has occupied an exceptional position in heterocyclic chemistry, and its derivatives have fascinated considerable interests in recent years for their versatile properties in chemistry and pharmacology. β- carboline is a modern artist of current drug discovery architectures. However, in the last 50 years, with the introduction of different biological evaluation, the importance of β- carboline scaffold for drug discovery has been recognized and considerable efforts from both academic and industrial researchers have been focused especially on the design and development of natural product inspire divers β- carboline scaffold.
Thus, the purpose of the present book is to provide a succinct summary of methods for the synthesis of various natural products to inspire diverse β- carboline scaffolds and their biological evaluation. I trust that both undergraduate and graduate students, researchers and faculties will nd in these pages an interesting guide and an updated state of the art on the enormous β- carboline scaffold.
Editor
Prof. Keshav Lalit Ameta
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About the Editor
Keshav Lalit Ameta is working as a Professor at the Department of Applied Chemistry, School of Applied material Sciences, Central University of Gujarat, Gandhinagar, India. Prior to the current position, he has served at Sardar Patel University, Vallabh Vidyanagar, Gujarat and Mody University of Science and Technology, Lakshmangarh, Rajasthan. Prof. Ameta has published over 100 research articles in the eld of organic chem-
istry and catalysis in the journals of international repute. He received his master and doctorate degree in Organic Chemistry from M. L. Sukhadia University, Udaipur, Rajasthan, India. He has vast experience of teaching both graduate and postgraduate level students. His research area involves synthesis, characterization and biological evaluation of different sized bioactive heterocyclic systems. In addition, to this he has keen interests in heterogeneous catalyzed organic synthesis and photocatalysis.
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