Article
Chemistry, Medicinal
Tongfei Jing, Zhijing Zhang, Zhenghui Kang, Jianshan Mo, Xiaotong Yue, Ziyou Lin, Xiang Fu, Chang Liu, Hang Ma, Xiaolei Zhang, Wenhao Hu
Summary: A series of novel compounds were designed, synthesized, and evaluated as PD-1/PD-L1 inhibitors. The optimized compound (1S,2S)-A25 showed potent inhibitory activity against PD-1/PD-L1 interaction and exhibited favorable pharmacokinetic properties and antitumor potency. It also suppressed tumor growth by activating the immune microenvironment, revealing its potential as a lead compound for further development of PD-1/PD-L1 inhibitors.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Organic
Desagoni Madhu, Vatsala Rani Jetti, Banda Narsaiah, Nagender Punna
Summary: In this study, tailored 3-trifluoroacetyl-quinolin-2(1H)-ones were used as carbonyl and acid surrogates in Passerini- and Ugi-type reactions to synthesize alpha-trifluoromethyl-alpha-hydroxy carboxamides and alpha-trifluoromethyl alpha-amino acids, achieving high yields under mild reaction conditions via an exocyclic carboximidate intermediate. The amide group in compound 1 acted as both an acid component and a reversible oxygen nucleophile to facilitate the reaction.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Organic
Asit Ghosh, Yuriy B. Lipisa, Natalia Fridman, Alex M. Szpilman
Summary: 2-Nitrocyclopropanes with various functional groups can be obtained as single diastereoisomers in one step by introducing ketones, amides, esters, and carboxylic acids at the 1 position of corresponding unsaturated carbonyl compounds using nitromethane as the nitromethylene component. The reaction proceeds at room temperature under mild conditions and the products can be further transformed into cyclopropyl-amino acids, among others. Nitrocyclopropanes and aminocyclopropanes are important structural motifs found in biologically active compounds and natural products.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Yuan Fei, Zhao Yan, Guo Qingsong, Yin Fudan, Lai Jinrong, Nian Beifang, Zhang Ming, Tang E
Summary: A new one-pot method for the efficient synthesis of 1-(1-(amino)cyclopropyl)ketone compounds has been developed. This method features mild reaction conditions, simple experiment operation, and good functional group compatibility.
CHINESE JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Qi Wang, Bixi Tang, Dandan Sun, Ying Dong, Yinchun Ji, Huanyu Shi, Liwei Zhou, Yueyue Yang, Menglan Luo, Qian Tan, Lin Chen, Yue Dong, Cong Li, Rongrong Xie, Yi Zang, Jingkang Shen, Bing Xiong, Jia Li, Danqi Chen
Summary: Idiopathic pulmonary fibrosis (IPF) is a serious chronic lung disease with inaccurate diagnosis, limited clinical therapy, and high mortality. The discoidin domain receptors (DDR) have been identified as promising drug targets for IPF treatment, and compound 47 shows potential as a candidate for further drug development.
ACTA PHARMACEUTICA SINICA B
(2022)
Article
Chemistry, Applied
Dirgha Raj Joshi, Ikyon Kim
Summary: In this study, a modular approach was used to synthesize a wide range of 1-cyano-3-(hetero)arylindolizines through aldol-cyclopropanation-oxidative cycloisomerization. DDQ was utilized for the first time to selectively synthesize the pyrrole units from cyclopropyl pyridines. The regioselective oxidation of the benzylic position by DDQ enabled the access to one regioisomer out of two possible ones. Additionally, homo-dimerization at the C2, C5, or C7 sites of indolizines in the presence of DDQ was discovered for the first time.
ADVANCED SYNTHESIS & CATALYSIS
(2022)
Article
Chemistry, Multidisciplinary
Ranjay Shaw, Prasoon Prakash, Ismail Althagafi, Nand Gopal Giri, Ramendra Pratap
Summary: A simple and efficient approach was developed to synthesize multifunctional phenols via the 1,3-dianionic annulation of acetone. Different substituted ketones were used to obtain a variety of phenolic compounds. The structure of one compound was confirmed using the single-crystal X-ray approach.
Article
Biotechnology & Applied Microbiology
Amol Gulab Khatik, Abhijeet Bhimrao Muley, Pavankumar Ramdas More, Arvind Kumar Jain
Summary: This study screened transaminases capable of carrying out chiral selective transamination of 1-(3-methylphenyl)ethan-1-one to (1R)-(3-methylphenyl)ethan-1-amine and found that ATA-025 was the best enzyme and dimethylsulfoxide was the best co-solvent. By optimizing variables such as enzyme loading, substrate loading, temperature, and pH, the study achieved maximum conversion, good product formation, and higher yield. The green and novel enzymatic approach using the optimized process can be used for the synthesis of different active pharma entities.
BIOPROCESS AND BIOSYSTEMS ENGINEERING
(2023)
Article
Chemistry, Multidisciplinary
Jie Shen, Ruijuan Ye, Huaqiang Zeng
Summary: A strategy for generating heteromeric peptidic ensembles via a crystal packing-inspired social self-sorting process is proposed. By modifying chain separation distances and adding special groups, highly stable hetero-oligomeric ensembles with alternated binding units are obtained.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Biochemistry & Molecular Biology
Maxim D. D. Gotsko, Ivan V. V. Saliy, Igor A. A. Ushakov, Lyubov N. N. Sobenina, Boris A. A. Trofimov
Summary: An efficient method for synthesizing pharmaceutically and high-tech prospective 2-(3-amino-2,4-dicyanophenyl)pyrroles has been developed. The method involves the reaction of easily available substituted acylethynylpyrroles with malononitrile, resulting in yields up to 88%. In some cases, the reaction direction changes, leading to unexpected product formation.
Article
Chemistry, Physical
Elisa Hernandez, Ruben Santiago, Cristian Moya, Pablo Navarro, Jose Palomar
Summary: This study proposes the use of amino acid based ionic liquids as catalysts to promote the conversion of CO2 with propylene oxide to produce propylene carbonate. Experimental results demonstrate that aa-ILs with higher CO2 absorption capacity can catalyze the reaction more effectively.
JOURNAL OF MOLECULAR LIQUIDS
(2021)
Article
Chemistry, Medicinal
Qi Lv, Xiang Pan, Dan Wang, Quanjin Rong, Ben Ma, Xiaolong Xie, Yinan Zhang, Junwei Wang, Lihong Hu
Summary: Inhibiting tumor-associated macrophages by blocking CSF-1/CSF-1R signal has become a promising strategy for cancer immunotherapy. A novel series of orally highly effective CSF-1R inhibitors were designed, among which compound 21 showed excellent inhibitory activity and potent antiproliferative effects against colorectal cancer cells. Additionally, compound 21 demonstrated superior efficacy over PLX3397 in vivo, making it a promising candidate for colorectal cancer immunotherapy.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Zaki Ahmed B. Munshi, Mubarak H. H. Shaikh, Pravinsing S. S. Girase, Iqrar Ahmad, Harun Patel, Bhata R. R. Chaudhari
Summary: We synthesized and characterized N-substituted derivatives of 1-cyclopropyl-6,7-difluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carbohydrazide and evaluated their antibacterial activity. We found that modification at the C-3 position decreases the activity of the quinolone scaffold. Docking studies with S. aureus DNA gyrase confirmed the binding interaction of the most active molecule, 5a, and in silico ADME prediction showed that all synthesized compounds met the criteria for being orally active drugs.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Article
Materials Science, Multidisciplinary
Amir Iqbal, Avneesh Mishra, Dorota Weglowska, Roman Dabrowski, Ravindra Dhar
Summary: Research on ferroelectric liquid crystals has shifted from being mainly focused on display devices and fast optical shutter elements to various fields such as spatial light modulators, optical sensors, polarisation gratings, and photonic and optical devices. This study investigated the thermodynamic, textural, electrical, and switching behavior of a highly tilted FLC material, confirming the presence of cholesteric, chiral smectic C, and hexatic phases in cooling cycle with temperature-dependent spontaneous polarization and rapid switching time. Conductivity of the material in these phases was also determined.
Article
Immunology
Muhammad Faheem, Yusuf S. Althobaiti, Abdul Waheed Khan, Arran Ullah, Syed Hussain Ali, Umair Ilyas
Summary: The study examined the effect of B3 in an animal model of acute epileptic shock. Results showed that B3 delayed the onset of seizures and increased the expression of protective enzymes while reducing inflammation markers in the cortex. B3 demonstrated neuroprotective effects and anticonvulsant effects mediated through GABAA pathways.
JOURNAL OF INFLAMMATION RESEARCH
(2021)
Article
Oncology
Jenny L. Pokorny, David Calligaris, Shiv K. Gupta, Dennis O. Iyekegbe, Dustin Mueller, Katrina K. Bakken, Brett L. Carlson, Mark A. Schroeder, Debra L. Evans, Zhenkun Lou, Paul A. Decker, Jeanette E. Eckel-Passow, Vincenzo Pucci, Bennett Ma, Stuart D. Shumway, William F. Elmquist, Nathalie Y. R. Agar, Jann N. Sarkaria
CLINICAL CANCER RESEARCH
(2015)
Article
Radiology, Nuclear Medicine & Medical Imaging
Eric D. Hostetler, Hong Fan, Aniket D. Joshi, Zhizhen Zeng, Waisi Eng, Liza Gantert, Marie Holahan, Xianjun Meng, Patricia Miller, Stacey O'Malley, Mona Purcell, Kerry Riffel, Cristian Salinas, Mangay Williams, Bennett Ma, Nicole Buist, Sean M. Smith, Paul J. Coleman, Christopher D. Cox, Brock A. Flores, Izzat T. Raheem, Jacquelynn J. Cook, Jeffrey L. Evelhoch
MOLECULAR IMAGING AND BIOLOGY
(2016)
Article
Chemistry, Medicinal
Izzat T. Raheem, John D. Schreier, Joy Fuerst, Liza Gantert, Eric D. Hostetler, Sarah Huszar, Aniket Joshi, Monika Kandebo, Somang H. Kim, Jing Li, Bennett Ma, Georgia McGaughey, Sujata Sharma, William D. Shipe, Jason Uslaner, George H. Vandeveer, Youwei Yan, John J. Renger, Sean M. Smith, Paul J. Coleman, Christopher D. Cox
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2016)
Article
Pharmacology & Pharmacy
Bennett Ma, Roy Eisenhandler, Yuhsin Kuo, Paul Rearden, Ying Li, Peter J. Manley, Sheri Smith, Karsten Menzel
EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS
(2017)
Article
Pharmacology & Pharmacy
Bennett Ma, Bin Luo, Danielle H. Euler, Tara E. Cusick, Gregg Wesolowski, Helmut Glantschnig, Le T. Duong, Yangsi Ou, Steven S. Carroll, Laura S. Lubbers
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2017)
Article
Pharmacology & Pharmacy
Bennett Ma, Aline Barth, Carolyn M. McHale, Ming-Tain Lai
ANTIVIRAL RESEARCH
(2018)
Article
Chemistry, Medicinal
Scott E. Wolkenberg, Zhijian Zhao, David D. Wisnoski, William H. Leister, Julie O'Brien, Wei Lemaire, David L. Williams, Marlene A. Jacobson, Cyrille Sur, Gene G. Kinney, Doug J. Pettibone, Philip R. Tiller, Sheri Smith, Christopher Gibson, Bennett K. Ma, Stacey L. Polsky-Fisher, Craig W. Lindsley, George D. Hartman
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2009)
Article
Chemistry, Medicinal
Izzat T. Raheem, Michael J. Breslin, Christine Fandozzi, Joy Fuerst, Nicole Hill, Sarah Huszar, Monika Kandebo, Somang H. Kim, Bennett Ma, Georgia McGaughey, John J. Renger, John D. Schreier, Sujata Sharma, Sean Smith, Jason Uslaner, Youwei Yan, Paul J. Coleman, Christopher D. Cox
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2012)
Article
Pharmacology & Pharmacy
Cheri M. Maciolek, Bennett Ma, Karsten Menzel, Sebastien Laliberte, Kevin Bateman, Paul Krolikowski, Christoper R. Gibson
DRUG METABOLISM AND DISPOSITION
(2011)
Article
Cardiac & Cardiovascular Systems
Philip E. Brandish, Thomas W. Forest, Hongxing Chen, Nicholas T. Gatto, Sylvain Molon-Noblot, Izabela Zwierzynski, Peter Szczerba, Gary E. Adamson, Bennett K. Ma, Osvaldo A. Flores, James C. Hershey
JOURNAL OF CARDIOVASCULAR PHARMACOLOGY
(2009)
Article
Pharmacology & Pharmacy
Bennett Ma, Stacey L. Polsky-Fisher, Stanley Vickers, Donghui Cui, A. David Rodrigues
DRUG METABOLISM AND DISPOSITION
(2007)
Article
Biochemistry & Molecular Biology
Bennett Ma, Frank N. Chang
Article
Pharmacology & Pharmacy
CY Tang, B Ma
DRUG METABOLISM AND DISPOSITION
(2005)
Article
Chemistry, Medicinal
Bennett Ma, Brian A. Carr, Paul Krolikowski, Frank N. Chang
CHEMICAL RESEARCH IN TOXICOLOGY
(2007)