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Chemistry, Organic
Nikita A. Kaminskiy, Ekaterina E. Galenko, Mariya A. Kryukova, Mikhail S. Novikov, Alexander F. Khlebnikov
Summary: This study discovered that alpha-diazopyrroles selectively react with enamines at room temperature to produce organic compounds, which can be used for the synthesis of functionalized heterocycles.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Oncology
Abel Tesfaye Anshabo, Laychiluh Bantie, Sarah Diab, Jimma Lenjisa, Alemwork Kebede, Yi Long, Gary Heinemann, Jasmine Karanjia, Benjamin Noll, Sunita K. C. Basnet, Manjun Li, Robert Milne, Hugo Albrecht, Shudong Wang
Summary: CDDD11-8 is an orally bioactive inhibitor of CDK9 that can suppress leukemia cell proliferation and inhibit tumor growth by synergistically inhibiting FLT3. It has the potential to overcome FLT3 inhibition resistance by blocking the upregulation of cancer cell-survival genes.
Article
Chemistry, Medicinal
Veronica Calvo, David Surguladze, An-Hu Li, Matthew D. Surman, Srikanth Malibhatla, Madhavarao Bandaru, Suresh Krishna Jonnalagadda, Ravi Adarasandi, Madhusudhan Velmala, Durga Rama Prasad Singireddi, Mahendar Velpuri, Bhaskar Reddy Nareddy, Visweswara Sastry, Chiranjeevi Mandati, Rambabu Guguloth, Shapi Siddiqui, Basanagoud S. Patil, Elena Chad, Jennifer Wolfley, Jennifer Gasparek, Kirsten Feldman, Matthew Betzenhauser, Brent Wiens, Mary Koszelak-Rosenblum, Guangyu Zhu, Hongwen Du, Alan C. Rigby, Mark J. Mulvihill
Summary: In this study, a series of potent, selective, and orally bioavailable PERK inhibitors were identified, with compound (28) showing robust pharmacokinetics and significant tumor growth inhibition in a renal cell carcinoma xenograft model. This compound warrants further investigation as a tool compound for mechanistic studies.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Multidisciplinary
Juraj Galeta, Veronika Slachtova, Martin Dracinsky, Milan Vrabel
Summary: A synthetic strategy for the formation of pyrrolo[2,1-f][1,2,4]triazines is presented. It is shown that various readily available 1,2,4-triazines can be efficiently alkylated under mild conditions to yield 1-alkyl-1,2,4-triazinium salts. These stable salts can serve as precursors for triazinium ylides, which undergo 1,3-dipolar cycloadditions with electron-poor dipolarophiles to afford polysubstituted pyrrolotriazines in a single step.
Article
Pharmacology & Pharmacy
Silvi A. Chacko, Wu Yang, Yufeng Wang, Yuan Tian, Yang Hong, Michael Wallace, Bonnie Wang, William R. Ewing, Joseph M. Luettgen, Yue-Zhong Shu, Lisa J. Christopher
Summary: The study found that FXIa-6f is mainly cleared through metabolic pathways in preclinical species, with most drug-related materials excreted through bile, including oxidative metabolites on the macrcycle or P1 region, descarbamoylation of the methyl carbamate side chain, and a glutathione conjugate on the 2,6-difluoro-3-chlorophenyl ring. Although the parent drug was the primary drug-related component in circulation in all preclinical species, the species differences in the observed metabolic pathways in vitro were reflected in the plasma.
Article
Chemistry, Medicinal
Shuai Wang, Sai-Qi Wang, Qiu-Xu Teng, Zi-Ning Lei, Zhe-Sheng Chen, Xiao-Bing Chen, Hong-Min Liu, Bin Yu
Summary: The triazolo[1,5-a]pyrimidine derivative WS-898 was discovered as a highly effective ABCB1 inhibitor capable of reversing PTX resistance in cells. WS-898 inhibited the efflux function of ABCB1, leading to increased intracellular PTX concentration and enhanced drug efficacy. Additionally, WS-898 showed promising results in in vivo PTX sensitization without causing obvious toxicity.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Hao-Yue Xiang, Xiang Wang, Yan-Hong Chen, Xi Zhang, Cun Tan, Yi Wang, Yi Su, Zhi-Wei Gao, Xiao-Yan Chen, Bing Xiong, Zhao-Bing Gao, Yi Chen, Jian Ding, Ling-Hua Meng, Chun-Hao Yang
Summary: The PI3Ks pathway is commonly dysregulated in human cancers, making it a promising target for anti-cancer drugs. Compound 37 (CYH33) was identified as a selective PI3Ka inhibitor with potential anti-cancer properties, inhibiting phosphorylation of AKT to modulate the PI3K/AKT/mTOR pathway in human cancer cells. Evaluation in vivo against SKOV-3 xenograft models demonstrated dose-dependent antitumor efficacy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Yi Shen, Craig A. Zificsak, Jill E. Shea, Xuegang Lao, Oana Bollt, Xiufen Li, Joseph G. Lisko, Jay P. Theroff, Courtney L. Scaife, Mark A. Ator, Bruce A. Ruggeri, Bruce D. Dorsey, Scott K. Kuwada
JOURNAL OF MEDICINAL CHEMISTRY
(2015)
Article
Biochemistry & Molecular Biology
Karen L. Milkiewicz, Linda R. Weinberg, Mark S. Albom, Thelma S. Angeles, Mangeng Cheng, Arup K. Ghose, Renee C. Roemmele, Jay P. Theroff, Ted L. Underiner, Craig A. Zificsak, Bruce D. Dorsey
BIOORGANIC & MEDICINAL CHEMISTRY
(2010)
Article
Chemistry, Medicinal
Craig A. Zificsak, Jay P. Theroff, Lisa D. Aimone, Mark S. Albom, Thelma S. Angeles, Rebecca A. Brown, Deborah Galinis, Jennifer V. Grobelny, Torsten Herbertz, Jean Husten, Laura S. Kocsis, Christine LoSardo, Sheila J. Miknyoczki, Seetha Murthy, Damaris Rolon-Steele, Ted L. Underiner, Kevin J. Wells-Knecht, Candace S. Worrell, Kelli S. Zeigler, Bruce D. Dorsey
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2011)
Article
Chemistry, Medicinal
Craig A. Zificsak, Jay P. Theroff, Lisa D. Aimone, Thelma S. Angeles, Mark S. Albom, Mangeng Cheng, Eugen F. Mesaros, Gregory R. Ott, Matthew R. Quail, Ted L. Underiner, Weihua Wan, Bruce D. Dorsey
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2011)
Article
Chemistry, Medicinal
Linda R. Weinberg, Mark S. Albom, Thelma S. Angeles, Jean Husten, Joseph G. Lisko, Robert J. McHugh, Karen L. Milkiewicz, Seetha Murthy, Gregory R. Ott, Jay P. Theroff, Rabindranath Tripathy, Ted L. Underiner, Craig A. Zificsak, Bruce D. Dorsey
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2011)
Article
Chemistry, Medicinal
Craig A. Zificsak, Diane E. Gingrich, Henry J. Breslin, Derek D. Dunn, Karen L. Milkiewicz, Jay P. Theroff, Tho V. Thieu, Ted L. Underiner, Linda R. Weinberg, Lisa D. Aimone, Mark S. Albom, Jennifer L. Mason, Lisa Saville, Jean Husten, Thelma S. Angeles, James P. Finn, Mahfuza Jan, Teresa M. O'Kane, Pawel Dobrzanski, Bruce D. Dorsey
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2012)
Article
Chemistry, Medicinal
Craig A. Zificsak, Yi Shen, Joseph G. Lisko, Jay P. Theroff, Xuegang Lao, Oana Bollt, Xiufen Li, Bruce D. Dorsey, Scott K. Kuwada
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2012)
Article
Chemistry, Organic
Changhong Ko, Richard P. Hsung, Ziyad F. Al-Rashid, John B. Feltenberger, Ting Lu, Jin-Haek Yang, Yonggang Wei, Craig A. Zificsak
Article
Chemistry, Organic
Craig R. Berry, Craig A. Zificsak, Alan C. Gibbs, Dennis J. Hlasta
Article
Chemistry, Organic
CA Zificsak, DJ Hlasta
TETRAHEDRON LETTERS
(2005)
Review
Chemistry, Organic
CA Zificsak, DJ Hlasta
Article
Chemistry, Organic
SJ Luo, CA Zificsak, RP Hsung
Article
Chemistry, Organic
JA Mulder, KCM Kurtz, RP Hsung, H Coverdale, MO Frederick, LC Shen, CA Zificsak
Article
Chemistry, Organic
N Sydorenko, CA Zificsak, AI Gerasyuto, RP Hsung
ORGANIC & BIOMOLECULAR CHEMISTRY
(2005)