10099-08-8Relevant articles and documents
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Sokol'skii,G.A. et al.
, (1971)
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Nickel-Catalyzed Enantioconvergent Reductive Hydroalkylation of Olefins with α-Heteroatom Phosphorus or Sulfur Alkyl Electrophiles
Fu, Yao,He, Shi-Jiang,Li, Yan,Lu, Xi,Wang, Jia-Wang,Wang, Xiao-Xu,Xu, Zhe-Yuan
supporting information, (2020/01/22)
Substantial advances in enantioconvergent C(sp3)-C(sp3) bond formation reactions have been made in recent years through the use of transition-metal-catalyzed cross-coupling reactions of racemic secondary alkyl electrophiles with organometallic reagents. Herein, we report a general process for the asymmetric construction of alkyl-alkyl bonds adjacent to heteroatoms, namely, a nickel-catalyzed enantioconvergent reductive hydroalkylation of olefins with α-heteroatom phosphorus or sulfur alkyl electrophiles. Including the use of readily available olefins, this reaction has considerable advantages, such as mild reaction conditions, a broad substrate scope, and good functional group compatibility, making it a desirable alternative to traditional electrophile-nucleophile cross-coupling reactions.
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides
Bonnet, Muriel,Hong, Cho Rong,Wong, Way Wua,Liew, Lydia P.,Shome, Avik,Wang, Jingli,Gu, Yongchuan,Stevenson, Ralph J.,Qi, Wen,Anderson, Robert F.,Pruijn, Frederik B.,Wilson, William R.,Jamieson, Stephen M. F.,Hicks, Kevin O.,Hay, Michael P.
supporting information, p. 1241 - 1254 (2018/02/17)
Innovations in the field of radiotherapy such as stereotactic body radiotherapy, along with the advent of radio-immuno-oncology, herald new opportunities for classical oxygen-mimetic radiosensitizers. The role of hypoxic tumor cells in resistance to radiotherapy and in suppression of immune response continues to endorse tumor hypoxia as a bona fide, yet largely untapped, drug target. Only nimorazole is used clinically as a radiosensitizer, and there is a dearth of new radiosensitizers in development. Here we present a survey of novel nitroimidazole alkylsulfonamides and document their cytotoxicity and ability to radiosensitize anoxic tumor cells in vitro. We use a phosphate prodrug approach to increase aqueous solubility and to improve tumor drug delivery. A 2-nitroimidazole and a 5-nitroimidazole analogue demonstrated marked tumor radiosensitization in either ex vivo assays of surviving clonogens or tumor regrowth delay.