Article
Chemistry, Multidisciplinary
Rajpratap Kshatriya, Premchand Shelke, Suraj Mali, Gauravi Yashwantrao, Amit Pratap, Satyajit Saha
Summary: This study describes the design, synthesis, and evaluation of pyrazolone ring-appended triarylmethanes with anticancer properties, using p-TSA catalyst for condensation reactions. Some synthesized molecules showed significant anticancer activity, indicating a potential direction for the development of anticancer molecules.
Review
Chemistry, Medicinal
Gulshan Kumar, Ravi Shankar
Summary: Isoxazolines are nitrogen- and oxygen-containing five-membered heterocyclic scaffolds with extensive biological activities. They can be readily synthesized through 1,3-dipolar cycloaddition and have played a role in enhancing the biological activity of natural products and synthetic compounds.
Review
Chemistry, Physical
Swati Pawar, Mukesh Kumar Kumawat, Monika Kundu, Kapil Kumar
Summary: Leishmaniasis is a common neglected tropical disease that affects over 98 countries and millions of people each year. It poses severe risks to the genetic inheritance and host immunity of over one billion individuals. Currently, there is no specific treatment available, thus there is an urgent need for novel therapies. This review presents the synthesis of various compounds that show great potential against leishmaniasis and its causative species, providing insights for new drug development.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Review
Chemistry, Multidisciplinary
Heba E. Hashem, Youness El Bakri
Summary: This article mainly discusses the synthetic methods of benzimidazole derivatives and their biological importance.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Shanshan Zhang, Yi Liu, Ansar Javeed, Cuiqin Jian, Jinlyu Sun, Shandong Wu, Bingnan Han
Summary: The prevalence of allergic diseases has been increasing globally, affecting approximately 20-30% of the population. The challenge in anti-allergy research lies in developing drugs with high efficacy and minimal side effects by targeting multiple mechanisms based on different clinical characteristics and allergens. This review highlights potential therapeutic targets and synthetic small molecules for anti-allergy treatment, focusing on the structure-activity relationship and mechanism of compound-target interaction. The findings can contribute to the improvement of virtual screening efficiency for antiallergic drug development and serve as a valuable reference for related research areas such as allergy, inflammation, and cancer drug design.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Sanjay Singh, Sankalan Mondal, Nagaraju Vodnala, Chinmoy Kumar Hazra
Summary: In this study, unsymmetrical polyarylated alkanes were synthesized using a cheap, commercially available Bronsted acid-catalytic system (pTSA center dot H2O)/HFIP. The one-pot three-component approach avoided the use of pyrophoric reagents, metal catalysts, toxic solvents, or Grignard reagents, and showed high greenness in terms of various green metrics. The method was also applied for the synthesis of pharmaceuticals and natural product functionalization.
Review
Chemistry, Multidisciplinary
Fabrizio Ortu
Summary: This review provides an overview of the important starting materials and ligands used in rare earth synthetic chemistry, covering their preparations and applications in modern synthetic methodologies.
Review
Oncology
Pooja Ratre, Swanand Kulkarni, Sweety Das, Chengyuan Liang, Pradyumna Kumar Mishra, Suresh Thareja
Summary: This review provides an overview of coumarin as an ideal template for designing novel anti-breast cancer compounds and discusses the diversity of coumarin as a target for aromatase. The structure-activity relationship analysis of coumarin core is summarized to identify the essential pharmacophoric features for developing aromatase inhibitors. The review also covers key synthesis techniques to aid in designing and developing analogues with significant anti-breast cancer properties.
Review
Biochemistry & Molecular Biology
Srinivas Reddy Merugu, Srinivasulu Cherukupalli, Rajshekhar Karpoormath
Summary: [1,2,4]Triazolo[1,5-a]pyrimidine is an important heterocyclic scaffold known for its broad range of pharmacological activities, and several marketed drugs have demonstrated its potential in medicinal chemistry. This review provides an overview of the synthetic strategies and pharmacological applications of differently substituted [1,2,4]triazolo[1,5-a]pyrimidine, with a focus on structure-activity relationship studies.
CHEMISTRY & BIODIVERSITY
(2022)
Review
Chemistry, Inorganic & Nuclear
Adeena Asif, Rana Yasir Nadeem, Muhammad Adnan Iqbal, Shamsa Bibi, Muhammad Irfan
Summary: Organometallic complexes of neodymium exhibit unique coordinating ability, suitable for applications in luminescence, catalysis, biology, and magnetism, and can be synthesized through various routes.
REVIEWS IN INORGANIC CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Yuko Kinowaki, Towako Taguchi, Iichiroh Onishi, Susumu Kirimura, Masanobu Kitagawa, Kouhei Yamamoto
Summary: Ferroptosis is a type of iron-dependent, non-apoptotic cell death that sensitizes drug-resistant tumors and cancer stem cells. Synthetic lethal strategies, targeting mechanisms not directly addressed by conventional therapies, show potential for specific malignant cells with low toxicity and possible new drug combinations. The research focuses on exploring ferroptosis-related molecules and synthetic lethality for potential therapeutic targets.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Multidisciplinary
Ze-Xin Zhang, Michael C. Willis
Summary: Sulfonamides, with their unique structure and properties, play a significant role in designing bioactive molecules. Mono aza variants, sulfonimidamides, and double aza analogs, sulfondiimidamides, are two functional groups. However, the synthesis of sulfondiimidamides is challenging, and their assembly and modification can be achieved through specific methods.
Review
Chemistry, Medicinal
Miguel Maia, Diana I. S. P. Resende, Fernando Duraes, Madalena M. M. Pinto, Emilia Sousa
Summary: Xanthenes and its derivatives, similar to xanthones, have diverse biological applications. This review summarizes the synthetic methodologies for obtaining xanthenes from simple starting materials or modification of related structures, as well as their biological activities and safety considerations.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Rakesh Pahwa, Jatin Chhabra, Raj Kumar, Rakesh Narang
Summary: This paper discusses key approaches to address resistance associated with melphalan, as well as chemical and formulation developments to enhance its characteristics and targeted profile. The rationale of the article also summarizes recent analytical methods, structure-activity relationship, pharmacokinetics, interactions, potential adverse effects, and medicinal updates of melphalan, including synthetic developments, derivatives, conjugates, and prodrugs, along with encouraging insights and research findings.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Ramandeep Kaur, Kapil Kumar
Summary: Quinoline scaffold plays a crucial role in medicinal agents, exhibiting useful biological activities such as anticancer and antibacterial properties. Despite various synthetic strategies developed worldwide, limitations such as side product formation and the use of expensive metal catalysts still exist, prompting ongoing efforts to develop efficient and cost-effective synthetic protocols.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Multidisciplinary
Deblina Roy, Gautam Panda
Article
Chemistry, Organic
Amit Kumar, Gautam Panda
Summary: In this study, a novel reaction method utilizing Magnesium chloride (MgCl2) catalysis was successfully developed for the highly C3-selective ring-opening reaction of 2,3-epoxy alcohols with N-nucleophiles and sodium azide. The reaction proceeded under mild conditions and showed high yields of the desired 3-amino-1,2 diols and 3-azido-1,2 diols, demonstrating practicality and broad functional group tolerance.
TETRAHEDRON LETTERS
(2021)
Article
Chemistry, Physical
Deblina Roy, Kasim Ali, Gautam Panda
Summary: The study reveals a method using Wilkinson catalyst for hydroacylation simplifies the synthesis of bedaquiline analogs with reduction of steps. Direct installation of three crucial aryl rings in the reaction leads to a series of bedaquiline analogs.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Multidisciplinary
Deblina Roy, Grace Kaul, Abdul Akhir, Ashok Kumar Sharma, Satyen Saha, Sidharth Chopra, Gautam Panda
Summary: A library of diarylmethyl amines targeting ESKAPE bacterial pathogens was synthesized, and compounds with potent antibacterial activity against Gram-positive bacteria were identified. The presence of lipophilic and nitrogenous components was found to be important for antibacterial activity.
Article
Chemistry, Organic
Amit Kumar, Gaurav Sharma, Sanjeev K. Shukla, Gautam Panda
Summary: A tandem reaction involving semipinacol rearrangement and aldehyde arylation or alkylation has been discovered. This reaction allows for the formation of functionalized 1,3-diols bearing three consecutive tertiary stereocenters from various trisubstituted 2,3-epoxy alcohols and Grignard reagents. The resulting 1,3-diols are confirmed to exist in the anti configuration.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Amit Kumar, Neetu Kumari, Sandeep Bhattacherjee, Umamageswaran Venugopal, Shahid Parwez, Mohammad Imran Siddiqi, Manju Y. Krishnan, Gautam Panda
Summary: Novel chemical compounds were discovered to inhibit the bc1 complex mutant of Mycobacterium tuberculosis, with two molecules showing MICs of 8 and 16 mu M, compared to MICs of 128 and 256 mu M against the wild type. These compounds were bactericidal to wild type bacteria under hypoxic conditions at concentrations much lower than their MICs, and showed synergy with an inhibitor of the bc1 complex in inhibiting bacterial growth.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Kasim Ali, Gautam Panda
Summary: An efficient transition-metal-free multicomponent approach to the regioselective synthesis of highly substituted N-alkylpyrazoles through 1,6-addition of pyrazole (in situ generated from alpha,beta-unsaturated aldehyde and hydrazide) to para-Quinone Methides has been developed. The N-alkylpyrazole containing triarylmethanes having several heteroaryl rings (quinoline, pyridine, thiophene) at the central methine carbon atom was developed. This chemical process may be used for large-scale synthesis and provides a novel way to produce triarylmethanes with diverse functional groups.
CHEMISTRY-AN ASIAN JOURNAL
(2023)
Review
Chemistry, Medicinal
Indranil Chatterjee, Kasim Ali, Gautam Panda
Summary: This review critically analyzes the synthetic strategies and anticancer activities of benzoxazines and benzoxazepines compounds reported from 2010 onwards. The structure-activity relationship of the benzoxazine and benzoxazepine scaffolds containing bioactive compounds is also studied, focusing on how structural modification affects their anticancer activity.
Review
Chemistry, Multidisciplinary
Arpita Banerjee, Indranil Chatterjee, Gautam Panda
Summary: This article discusses the significance of tyrosine as a chiral pool in the synthesis of alkaloids, and compares synthetic steps, overall yield, and other factors between tyrosine-based and non-tyrosine-based routes.
Article
Chemistry, Multidisciplinary
Saroj Maji, Souvik Barman, Gautam Panda
Summary: In this study, a novel synthetic route towards nintedanib was developed using a stereoselective intramolecular cyclization strategy to convert beta-keto amide into a 3-acyloxindole derivative, an important scaffold for nintedanib synthesis. The condensation of the oxindole scaffold with a synthesized amine derivative led to the successful synthesis of nintedanib.
Article
Chemistry, Organic
Indranil Chatterjee, Gautam Panda
Summary: This paper describes a palladium-catalyzed regioselective reaction of propargylic carbonate with thiophenols and benzene selenol. The addition of thiols to propargylic carbonates provides an atom-economic and effective process. The reaction proceeds through hydrothiolation to produce mono(arylthiol) alkenes and hydrothiolation followed by Tsuji-Trost type substitution to form bis(arylthiol) alkenes by controlling the equivalence of thiophenols. This coupling reaction exhibits good tolerance towards functional groups and leads to the formation of highly functionalized alkenylation products via the formation of new C-S and C-Se bonds.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2023)
Article
Chemistry, Organic
Kasim Ali, Indranil Chatterjee, Gautam Panda
Summary: A simple and efficient metal-free approach was developed for synthesizing 4-thio-substituted chroman and diarylmethyl thioethers, providing good yields and tolerance for labile functional groups. This method is applicable to large-scale synthesis.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2023)
Article
Chemistry, Organic
Kasim Ali, Gurudayal Prajapati, Ravi Sankar Ampapathi, Gautam Panda
Summary: The reductive coupling between allylic sulfonylhydrazones and aryl boronic acids can efficiently generate 1,3-diarylpropene systems under mild reaction conditions.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2022)
Article
Chemistry, Organic
Arpita Banerjee, Gautam Panda
Summary: In this study, a base mediated, transition metal-free intermolecular epoxide ring opening reaction followed by intramolecular aromatic nucleophilic substitution (SNAr) was developed to synthesize separable diastereomers of selected benzo[b][1,4,5]oxathiazepine 1-oxides. This strategy allows the formation of both C-N and C-O bonds simultaneously in a single step. The method has a wide substrate scope, uses simple reaction conditions, and is applicable for synthesizing bioactive molecules with similar skeletons as benzoxathiazepine 1-oxides.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2022)
Review
Chemistry, Multidisciplinary
Kasim Ali, Prajjval Mishra, Awnish Kumar, Damodara N. Reddy, Sushobhan Chowdhury, Gautam Panda
Summary: In this article, the synthesis, structure-reactivity relationships, and synthetic applications of quinone methides are discussed. The formation of intermediates during bioactivation and potential chemical manifestations leading to toxicity in biological systems are also covered.
CHEMICAL COMMUNICATIONS
(2022)
