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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, microlming, 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 identication 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- inammatory 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 scientic research.
Wishing you a happy reading experience and scientic pursuits as abundant and
fullling 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 efcacy, fewer side effects, and unique methods of action benets 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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