Results 131 to 140 of about 10,109,694 (374)

Structure-Activity Relationship for the Oxadiazole Class of Antibiotics [PDF]

, 2015
The structure-activity relationship (SAR) for the newly discovered oxadiazole class of antibiotics is described with evaluation of 120 derivatives of the lead structure.
Antunes, Nuno T., Boudreau, Marc A., Chang, Mayland, Ding, Derong, Lastochkin, Elena, Leemans, Erika, Lichtenwalter, Katerina, Mobashery, Shahriar, O’Daniel, Peter I., Peng, Zhihong, Pi, Hualiang, Schroeder, Valerie A., Song, Wei, Spink, Edward, Suckow, Mark A., Testero, Sebastian Andres, Vakulenko, Sergei, Wolter, William R.   +17 more
core   +2 more sources

Addressing persistent challenges in digital image analysis of cancer tissue: resources developed from a hackathon

Molecular Oncology, EarlyView.
Large multidimensional digital images of cancer tissue are becoming prolific, but many challenges exist to automatically extract relevant information from them using computational tools. We describe publicly available resources that have been developed jointly by expert and non‐expert computational biologists working together during a virtual hackathon
Sandhya Prabhakaran, Clarence Yapp, Gregory J. Baker, Johanna Beyer, Young Hwan Chang, Allison L. Creason, Robert Krueger, Jeremy Muhlich, Nathan Heath Patterson, Kevin Sidak, Damir Sudar, Adam J. Taylor, Luke Ternes, Jakob Troidl, Xie Yubin, Artem Sokolov, Darren R. Tyson   +16 more
wiley   +1 more source

Structural insights and biological activities of flavonoids: Implications for novel applications

Food Frontiers
Flavonoids are a major class of polyphenolic compounds that occur naturally in plants and are widely distributed in various dietary products. Flavonoids exhibit prominent physicochemical properties and biological activities, thereby garnering ...
Sheng Tang, Botao Wang, Xin Liu, Wenxia Xi, Yuanyuan Yue, Xiang Tan, Junying Bai, Linhua Huang   +7 more
doaj   +1 more source

Structure–Activity Relationship for the 4(3H)-Quinazolinone Antibacterials

Journal of Medicinal Chemistry, 2016
We recently reported on the discovery of a novel antibacterial (2) with a 4(3H)-quinazolinone core. This discovery was made by in silico screening of 1.2 million compounds for binding to a penicillin-binding protein and the subsequent demonstration of ...
R. Bouley, Derong Ding, Zhihong Peng, M. Bastian, E. Lastochkin, Wei Song, M. Suckow, Valerie A. Schroeder, W. Wolter, S. Mobashery, Mayland Chang   +10 more
semanticscholar   +1 more source

Etoposide‐induced cancer cell death: roles of mitochondrial VDAC1 and calpain, and resistance mechanisms

Molecular Oncology, EarlyView.
The complex mode of action of the topoisomerase II inhibitor etoposide in triggering apoptosis involves several mechanisms: overexpression of the mitochondrial protein VDAC1, leading to its oligomerization and formation of a large channel that mediates the release of pro‐apoptotic protein; and overexpression of the apoptosis regulators p53, Bax, and ...
Aditya Karunanithi Nivedita, Varda Shoshan‐Barmatz   +1 more
wiley   +1 more source

Structure-Activity and Lipophilicity Relationships of Selected Antibacterial Natural Flavones and Flavanones of Chilean Flora

Molecules, 2017
In this study, we tested eight naturally-occurring flavonoids—three flavanones and five flavones—for their possible antibacterial properties against four Gram-positive and four Gram-negative bacteria.
Javier Echeverría, Julia Opazo, Leonora Mendoza, Alejandro Urzúa, Marcela Wilkens   +4 more
doaj   +1 more source

Antioxidant Structure–Activity Relationship Analysis of Five Dihydrochalcones

Molecules, 2018
The study determined the comparative antioxidant capacities of five similar dihydrochalcones: phloretin, phloridzin, trilobatin, neohesperidin dihydrochalcone, and naringin dihydrochalcone.
Xican Li, Ban Chen, Hong Xie, Yuhua He, D. Zhong, Dongfeng Chen   +5 more
semanticscholar   +1 more source

Stochastic variation in the FOXM1 transcription program mediates replication stress tolerance

Molecular Oncology, EarlyView.
Cellular heterogeneity is a major cause of drug resistance in cancer. Segeren et al. used single‐cell transcriptomics to investigate gene expression events that correlate with sensitivity to the DNA‐damaging drugs gemcitabine and prexasertib. They show that dampened expression of transcription factor FOXM1 and its target genes protected cells against ...
Hendrika A. Segeren, Kathryn A. Wierenga, Frank M. Riemers, Elsbeth A. van Liere, Bart Westendorp   +4 more
wiley   +1 more source

Synthesis and activity of novel indole derivatives as inhibitors of CD38

Acta Pharmaceutica Sinica B, 2013
CD38 is a multifunctional enzyme/receptor expressed in a variety of mammalian tissues, regulating a wide range of physiological functions. Beginning with the previously reported compound 1, an inhibitor of human CD38 NADase, we synthesized a series of ...
Dongying Wu, Kaiyiu Ting, Yaokai Duan, Na Li, Jianguo Li, Liangren Zhang, Honcheung Lee, Lihe Zhang   +7 more
doaj   +1 more source

Aminothiazoles as Potent and Selective Sirt2 Inhibitors: A Structure-Activity Relationship Study.

Journal of Medicinal Chemistry, 2016
Sirtuins are NAD(+)-dependent protein deacylases that cleave off acetyl but also other acyl groups from the ε-amino group of lysines in histones and other substrate proteins.
M. Schiedel, Tobias Rumpf, Berin Karaman, A. Lehotzky, J. Olah, S. Gerhardt, J. Ovádi, W. Sippl, O. Einsle, M. Jung   +9 more
semanticscholar   +1 more source