DOI: 10.1055/s-00000083

Synlett

Issue Small-Molecule MedChem · Volume · 2025 DOI: 10.1055/s-015-61587

Small Molecules in Medicinal Chemistry

  • Thaker, Aanal; Patel, Shrusti; Dey, Rajdeep; Shaw, Suman; Bhatt, Hardik; Patel, Bhumika; Chaube, Udit:

    Advancements in mTOR Inhibitors for Non-Small-Cell Lung Cancer: Mechanisms, Efficacy, and Future Perspectives

    Image for article: Advancements in mTOR Inhibitors for Non-Small-Cell Lung Cancer: Mechanisms, Efficacy, and Future Perspectives
  • Sanjaykumar, Randhe Siddhant; Basavaraj, Chavan Sagar; Arshad, Anam Sania Md.; Singh, Rohit; Mahindroo, Neeraj:

    A Decade of FDA-Approved Pharmacophore-Based Small Molecules: Advances in Medicinal Chemistry from 2014 to 2024

    Image for article: A Decade of FDA-Approved Pharmacophore-Based Small Molecules: Advances in Medicinal Chemistry from 2014 to 2024
  • Milokhov, Demyd S.; Pomalin, Mykhailo S.; Lutsiuk, Tetiana M.; Hys, Vasyl Y.; Virych, Pavlo A.; Poliudov, Anton O.; Popova, Maria V.; Shishkina, Svitlana V.; Volovenko, Yulian M.; Dobrydnev, Alexey V.:

    Benzo[d][1,2]thiazepin-5-one 3-Oxides: An Unexplored Scaffold with Anticancer Activity

    Image for article: Benzo[<i>d</i>][1,2]thiazepin-5-one 3-Oxides: An Unexplored Scaffold with Anticancer Activity
  • Candito, David A.; Simov, Vladimir; Liu, Ping; Ardolino, Michael J.; Martinot, Theodore; Lyons, Thomas; Qi, Ji; Yin, Jingjun; Hao, Jinglai; Hu, Bin; Chen, Meng; Zhang, Jun; Lam, Yu-hong; Fuller, Peter H.; Ellis, J. Michael; Maddess, Matthew:

    A Concise Synthesis of a Key Azabicyclo[2.1.1]hexane Building Block for N-Heteroaryl Indazole LRRK2 Kinase Inhibitors

    Image for article: A Concise Synthesis of a Key Azabicyclo[2.1.1]hexane Building Block for <i>N</i>-Heteroaryl Indazole LRRK2 Kinase Inhibitors
  • Kumar, Ch. N. S. Sai Pavan; Jayathirtha, Vaidya Rao:

    Bioactive Molecules via Morita–Baylis–Hillman Chemistry

    Image for article: Bioactive Molecules <i>via</i> Morita–Baylis–Hillman Chemistry
  • 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

    Image for article: Design, Synthesis, and Biological Evaluation of Thioether Steroids as Glucocorticoid Receptor Modulators
  • Sharma, Anu; Vadodariya, Palak K.; Vaddoriya, Vaidehi N.; Dhameliya, Tejas M.:

    Comprehensive Updates on Antitubercular Endeavors Identified in 2023

    Image for article: Comprehensive Updates on Antitubercular Endeavors Identified in 2023
  • Ito, Toshiya; Kinoshita, Kazutomo; Tomizawa, Masaki; Shinohara, Shojiro; Nishii, Hiroki; Tanaka, Hiroshi; Kuramoto, Shino; Oikawa, Nobuhiro:

    Development of a Novel Tropomyosin Receptor Kinase Inhibitor Based on Structure–Activity Relationships: Identification of a Promising Clinical Candidate

    Image for article: Development of a Novel Tropomyosin Receptor Kinase Inhibitor Based on Structure–Activity Relationships: Identification of a Promising Clinical Candidate
  • Das, Debojyoti; Sadhukhan, Juheli; Mandal, Pabitra; Pramanik, Smritimoy; Kabir, Alomgir Shah; Adhikari, Susanta Sekhar:

    Synthesis of Novel Coumarin-Appended Dihydrothiopyrimidinones and Evaluation of Their Binding Interactions with Bovine Serum Albumin

    Image for article: Synthesis of Novel Coumarin-Appended Dihydrothiopyrimidinones and Evaluation of Their Binding Interactions with Bovine Serum Albumin
  • 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

    Image for article: Analogues of the Potent and Selective ERβ Agonist <i>trans</i>-4-(4-Hydroxyphenyl)cyclohexanemethanol: Synthesis and Evaluation
  • Alaeddini, AmirHossein; Karimian, Somaye; Noori, Milad; Dastyafteh, Navid; Mohammadi-Khanaposhtani, Maryam; Ghomi, Minoo Khalili; Bararjanian, Morteza; Iraji, Aida; Javanshir, Shahrzad; Larijani, Bagher; Ranjbar, Parviz Rashidi; Mahdavi, Mohammad:

    Design, Synthesis, Enzymatic Inhibition, and Antioxidant Activity of New 4-Phenylpiperazin-phenoxy-1,2,3-triazol-acetamide Derivatives as Tyrosinase Inhibitors

    Image for article: Design, Synthesis, Enzymatic Inhibition, and Antioxidant Activity of New 4-Phenylpiperazin-phenoxy-1,2,3-triazol-acetamide Derivatives as Tyrosinase Inhibitors
  • Garg, Aakriti; Bhattacharya, Bireswar; Samanta, Uttam; Singha, Subhankar; Ghosh, Dipanjan; Bhowmik, Subhendu; Jaisankar, Parasuraman; Gupta, Sreya:

    Phototriggered Migration of Indole-Based Cationic Fluorophore from Mitochondria to Nucleolus in Live Cells

    Image for article: Phototriggered Migration of Indole-Based Cationic Fluorophore from Mitochondria to Nucleolus in Live Cells
  • 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

    Image for article: A Decade of Piperazine-Based Small Molecules Approved by U.S. FDA: Exploring the Medicinal Chemistry Impact of this Versatile Pharmacophore
  • Chandra, Devesh; Sachin, Sachin; Rav, Shourabh; Sharma, Upendra:

    Quinoline-Based FDA-Approved Drugs: Synthetic Route and Clinical Uses

    Image for article: Quinoline-Based FDA-Approved Drugs: Synthetic Route and 
Clinical Uses
  • 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

    Image for article: Synthesis of 5-Functionalized 1-(Hetero)Aryl-1,2-thiazine 1-Oxides through a CSIC Reaction Strategy
  • Shaw, Suman K.; Dey, Rajdeep; Yadav, Ruchi; Baldiwala, Aliasgar; Patel, Manan; Patel, Bhumika D.; Bhatt, Hardik G.; Natesan, Gopal; Jha, Abhishek; Chaube, Udit:

    Exploring Tetrahydroquinoline Derivatives: A New Frontier in Cancer Treatment

    Image for article: Exploring Tetrahydroquinoline Derivatives: A New Frontier in Cancer Treatment
  • Beveridge, Julia; Söderström, Marcus; Balestri, Lorenzo Jacopo Ilic; Prieto-Díaz, Rubén; Gutierrez-de-Teran, Hugo; Odell, Luke R; Hallberg, Mathias; Larhed, Mats; Gising, Johan:

    Benzylhydroxamic Acids as IRAP Inhibitors: Sulfonamide Variations

    Image for article: Benzylhydroxamic Acids as IRAP Inhibitors: Sulfonamide Variations
  • Roy, Sudipta; Kalita, Gitumoni; Maharana, Satyapriya; Chatterjee, Arunima; Jana, Rathin; Nath, Naba K.; Chatterjee, Paresh Nath:

    A Green Approach to 2-Amino-4H-chromenes by Calcium Lactate Catalyzed, One-Pot, Three-Component Reactions

    Image for article: A Green Approach to 2-Amino-4<i>H</i>-chromenes by Calcium Lactate Catalyzed, One-Pot, Three-Component Reactions
  • Khanka, Sonu; Rawat, Kundan S.; Pandey, Priyanka; Pal, Shyamal; Vats, Ravi P.; Rathur, Rajat; Sharma, Kriti; Dipali, Divya; Singh, Divya; Goel, Atul:

    An Efficient Synthesis of 3-Aryl-2H-chromene Derivatives as Potential Bone Anabolic Agents

    Image for article: An Efficient Synthesis of 3-Aryl-2<i>H</i>-chromene Derivatives as Potential Bone Anabolic Agents
  • 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

    Image for article: Hydrophilic α-Aryl-α-Diazoamides for Protein Esterification
  • 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

    Image for article: Oxaprozin and SB-431542 Hybrid Molecule Inhibits Fibrosis and Cancer Cell Migration
  • Toledano-Pinedo, Mireia; Diez-Iriepa, Daniel; Porro-Pérez, Alicia; Schäker-Hübner, Linda; Hanl, Maria; Samadi, Abdelouahid; Almendros, Pedro; Iriepa, Isabel; Rodríguez-Fernández, M. Mercedes; Griñán-Ferré, Christian; Siwek, Agata; Wolak, Małgorzata; Satała, Grzegorz; Bojarski, Andrzej J.; Doroż-Płonka, Agata; Handzlik, Jadwiga; Godyń, Justyna; Knez, Damijan; Gobec, Stanislav; Więckowska, Anna; Hansen, Finn K.; Marco-Contelles, José:

    Contilistat, a New Multitarget Small Polyfunctionalized Indole Derivative

    Image for article: Contilistat, a New Multitarget Small Polyfunctionalized Indole Derivative
  • 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

    Image for article: Structural Modifications for Biological Activity Enhancements in Thiosemicarbazone Scaffolds and Their Metal Complexes
  • Thien, Nguyen Duc; Ngoc, Hoang Kim; Nam, Nguyen-Hai; Anh, Duong Tien; Baecker, Daniel:

    A Novel Strategy for the Synthesis of N-Alkylated Oxindoles

    Image for article: A Novel Strategy for the Synthesis of N-Alkylated Oxindoles