Synlett

Issue 17 · October 2025

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Small Molecules in Medicinal Chemistry
2671
Tomohara, Keisuke; Nose, Takeru; Nambu, Hisanori:
Straightforward Synthesis of Unnatural α,α-Disubstituted α-Amino Acid Derivatives Using Readily Accessible Building Blocks

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2684
Nazir, Habiba; Naseer, Muhammad Moazzam:
The Isatin Scaffold: Exceptional Potential for the Design of Potent Bioactive Molecules

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2705
Kumar, Ankur; Debnath, Utsab; Roy, Kuldeep K.:
Thiazole-Scaffold-Based Anti-tubercular Agents: A Review on Synthesis and Structural Modifications

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2732
Khan, Tahmeena; Raza, Saman; Hashmi, Kulsum; Ahmad, Mohammad Imran; Khan, Abdul Rahman:
Structural Modifications for Biological Activity Enhancements in Thiosemicarbazone Scaffolds and Their Metal Complexes

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2763
Martinez, Alice K. de A.; Mourão, Penina S.; Corrêa, Arlene G.:
A Concise Account on Organocatalyzed Asymmetric Synthesis of Epoxide and Aziridine Derivatives from α,β-Unsaturated Carbonyl Compounds

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2772
Kumar, Ch. N. S. Sai Pavan; Jayathirtha, Vaidya Rao:
Bioactive Molecules via Morita–Baylis–Hillman Chemistry

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2791
Purohit, Priyank; Bhatt, Akanksha; Mittal, Ravi Kumar:
Ruthenium-Based Small-Molecule Complexes: A Promising Approach for Drug Discovery

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perspectives
Small Molecules in Medicinal Chemistry
2802
Goel, Kapil Kumar; Singhal, Peeush; Marianesan, Arockia Babu; Pandey, Sarvesh Kumar; Kumar, Roshan; Singh, Thakur Gurjeet; Tyagi, Yogita; Gaidhane, Shilpa; Singh, Mahendra Pratap; Dwivedi, Ashish Ranjan:
A Decade of Piperazine-Based Small Molecules Approved by U.S. FDA: Exploring the Medicinal Chemistry Impact of this Versatile Pharmacophore

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2819
Garg, Mansi; Verma, Ekta; Mishra, Shweta; Sahu, Adarsh:
Advancements in Isoniazid-Based Heterocyclic Derivatives as Potent Antitubercular Agents: A Comprehensive Review of Synthesis, SAR, and Biological Activity (2017–2023)

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2836
Kushwaha, Pragati; Rashi, Rashi; Bhardwaj, Ayush; Khan, Danish:
Advances in Synthesis and Anti-Alzheimer’s Disease Potential of Functionalized Benzofurans: A Recent Overview

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letter
Small Molecules in Medicinal Chemistry
2855
Dastari, Sowmya; Panda, Biswajit; Rasane, Sai; Reddyrajula, Rajkumar; Godugu, Chandraiah; Shankaraiah, Nagula:
Design, Synthesis, and In Vitro Cytotoxicity Studies of 1H-Benzimidazol-2-yl–Enaminone Hybrids as Tubulin Polymerization Inhibitors

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2864
Chakraborty, Kaustav; Dasgupta, Swagata; Pathak, Tanmaya:
Pyrimidine Carboxylic Acids Linked through 1,4,5-Trisubstituted 1,2,3-Triazoles: Synthesis and RNase A Inhibition Studies

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2869
Saliba, Paul; Hurem, David; Begovic, Lila; McNulty, James:
(Methylcarboxymethylene)tripropylphosphorane: A Stabilized Ylide for Rapid Formation of Methyl Vinyl Ketones and Applications in Medicinal Chemistry and Natural Product Synthesis

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2876
Chuchvera, Yaroslav O.; Korobka, Oleksandr P.; Horbatochkin, Yurii O.; Ostapchuk, Eugeniy N.; Popova, Maria V.; Shishkina, Svitlana V.; Volovenko, Yulian M.; Dobrydnev, Alexey V.:
Synthesis of 5-Functionalized 1-(Hetero)Aryl-1,2-thiazine 1-Oxides through a CSIC Reaction Strategy

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2883
Okon, Aniekan; Morgunov, Anton; Yang, Jinyi; Petri, Yana D.; Kilgore, Henry R.; Li, Yanfeng; Strieter, Eric R.; Raines, Ronald T.:
Hydrophilic α-Aryl-α-Diazoamides for Protein Esterification

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2890
Pumirat, Pattarapon; Sripraphot, Supang; Nilchan, Napon; Jiarpinitnun, Chutima:
Squaramide Homoserine Lactone Derivatives and their Abilities to Modulate Pseudomonas aeruginosa Biofilm Formation

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2895
Alzahrani, Abdullah Y. A.; El-Helw, Eman A. E.; Ramadan, Sayed K.:
Some Thiazolopyrimidine Derivatives: Synthesis, DFT, Cytotoxicity, and Pharmacokinetics Modeling Study

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2906
Gcabashe, Nontobeko; Kumar, Gobind; Seboletswe, Pule; Manhas, Neha; Singh, Parvesh:
A Rapid, Greener, and Sustainable Synthesis of N-Acylhydrazones of Isoniazid in a Deep-Eutectic Solvent

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2915
Sakamoto, Masaharu; Kai, Seriha; Tateishi, Hiroshi; Biswas, Tanima; Sakamoto, Takashi; Teshima, Misaki; Iwanaga, Misaki; Nishikawa, Akiko; Sakamoto, Arisa; Shimozono, Rie; Kameyama, Hiroki; Nambu, Masami; Masunaga, Takuya; Anraku, Kensaku; Fujita, Mikako; Otsuka, Masami:
Oxaprozin and SB-431542 Hybrid Molecule Inhibits Fibrosis and Cancer Cell Migration

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2920
Seaton, Wesley B.; West, Clayton; Burke, Susan J.; Schilletter, William A.; Tade, Opeyemi O.; Collier, J. Jason; Campagna, Shawn R.:
Design, Synthesis, and Biological Evaluation of Thioether Steroids as Glucocorticoid Receptor Modulators

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2925
Thien, Nguyen Duc; Ngoc, Hoang Kim; Nam, Nguyen-Hai; Anh, Duong Tien; Baecker, Daniel:
A Novel Strategy for the Synthesis of N-Alkylated Oxindoles

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2930
Rai, Aman; Soni, Arti; Bhatia, Rohit:
Design, Synthesis, and Molecular Docking Studies of Sulfonyl-Substituted Chromene Derivatives as Anticancer Agents

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2939
Ateşoğlu, Şeyma; Çakır, Furkan; Şenol, Ayşe Merve; Tokalı, Pelin; Şenol, Halil; Tokalı, Feyzi Sinan; Akbaş, Fahri; Kalay, Erbay:
Synthesis, Characterization and In Vitro and In Silico Biological Evaluation of New Mannich-Based Rhodanine and Thiazolidine-2,4-dione Derivatives as Potential Anti-Lung-Cancer Agents

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2948
Kobayakawa, Takuya; Yamamoto, Kenichi; Fukutome, Aiichiro; Arioka, Marisa; Tsuji, Kohei; Tamamura, Hirokazu:
Design and Synthesis of a C₂-Symmetric Cyclic Decapeptide and Its Peptidomimetic as Potential Inhibitors against Amyloid-β Aggregation

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2953
Ghosh, Priyam; Mukhopadhyay, Sayantani; Singh, Mrinalini; Ghosh, Siddhartha Sankar; Iyer, Parameswar Krishnan:
Exploring the Dual Therapeutic Potential of a Photoactivatable AIEgen in Cancer and Alzheimer’s Disease

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2960
Chaudhury, Subhabrata; Wetzel, Edward A.; Elmansy, Mohamed F.; Hanson, Alicia M.; Brown-Ford, Sandra; Gleason, Alexandra; Perera, K. L. Iresha Sampathi; Sem, Daniel S.; Donaldson, William A.:
Analogues of the Potent and Selective ERβ Agonist trans-4-(4-Hydroxyphenyl)cyclohexanemethanol: Synthesis and Evaluation

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2965
Pranathi, Abburi Naga; Devendra, Nagineni; Behera, Prakash Suman; Swetha, Yalavarthi Sai; Vasapalli, Kanchana; Misra, Sunil; Sridhar, Balasubramanian; Kantevari, Srinivas:
Three-Step Synthesis of 3-Aminoindole-2-carboxylate-Conjugated 2-Amino-6-chloropyrimidines and Their Anticancer Activity

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Synlett

Linked PDF of Table of Contents

Straightforward Synthesis of Unnatural α,α-Disubstituted α-Amino Acid Derivatives Using Readily Accessible Building Blocks

The Isatin Scaffold: Exceptional Potential for the Design of Potent Bioactive Molecules

Thiazole-Scaffold-Based Anti-tubercular Agents: A Review on Synthesis and Structural Modifications

Structural Modifications for Biological Activity Enhancements in Thiosemicarbazone Scaffolds and Their Metal Complexes

A Concise Account on Organocatalyzed Asymmetric Synthesis of Epoxide and Aziridine Derivatives from α,β-Unsaturated Carbonyl Compounds

Bioactive Molecules via Morita–Baylis–Hillman Chemistry

Ruthenium-Based Small-Molecule Complexes: A Promising Approach for Drug Discovery

A Decade of Piperazine-Based Small Molecules Approved by U.S. FDA: Exploring the Medicinal Chemistry Impact of this Versatile Pharmacophore

Advancements in Isoniazid-Based Heterocyclic Derivatives as Potent Antitubercular Agents: A Comprehensive Review of Synthesis, SAR, and Biological Activity (2017–2023)

Advances in Synthesis and Anti-Alzheimer’s Disease Potential of Functionalized Benzofurans: A Recent Overview

Design, Synthesis, and In Vitro Cytotoxicity Studies of 1H-Benzimidazol-2-yl–Enaminone Hybrids as Tubulin Polymerization Inhibitors

Pyrimidine Carboxylic Acids Linked through 1,4,5-Trisubstituted 1,2,3-Triazoles: Synthesis and RNase A Inhibition Studies

(Methylcarboxymethylene)tripropylphosphorane: A Stabilized Ylide for Rapid Formation of Methyl Vinyl Ketones and Applications in Medicinal Chemistry and Natural Product Synthesis

Synthesis of 5-Functionalized 1-(Hetero)Aryl-1,2-thiazine 1-Oxides through a CSIC Reaction Strategy

Hydrophilic α-Aryl-α-Diazoamides for Protein Esterification

Squaramide Homoserine Lactone Derivatives and their Abilities to Modulate Pseudomonas aeruginosa Biofilm Formation

Some Thiazolopyrimidine Derivatives: Synthesis, DFT, Cytotoxicity, and Pharmacokinetics Modeling Study

A Rapid, Greener, and Sustainable Synthesis of N-Acylhydrazones of Isoniazid in a Deep-Eutectic Solvent

Oxaprozin and SB-431542 Hybrid Molecule Inhibits Fibrosis and Cancer Cell Migration

Design, Synthesis, and Biological Evaluation of Thioether Steroids as Glucocorticoid Receptor Modulators

A Novel Strategy for the Synthesis of N-Alkylated Oxindoles

Design, Synthesis, and Molecular Docking Studies of Sulfonyl-Substituted Chromene Derivatives as Anticancer Agents

Synthesis, Characterization and In Vitro and In Silico Biological Evaluation of New Mannich-Based Rhodanine and Thiazolidine-2,4-dione Derivatives as Potential Anti-Lung-Cancer Agents

Design and Synthesis of a C₂-Symmetric Cyclic Decapeptide and Its Peptidomimetic as Potential Inhibitors against Amyloid-β Aggregation

Exploring the Dual Therapeutic Potential of a Photoactivatable AIEgen in Cancer and Alzheimer’s Disease

Analogues of the Potent and Selective ERβ Agonist trans-4-(4-Hydroxyphenyl)cyclohexanemethanol: Synthesis and Evaluation

Three-Step Synthesis of 3-Aminoindole-2-carboxylate-Conjugated 2-Amino-6-chloropyrimidines and Their Anticancer Activity