6248-20-0Relevant articles and documents
Cell-specific activation of gemcitabine by endogenous H2S stimulation and tracking through simultaneous fluorescence turn-on
Maiti, Mrinmoy,Yoon, Shin A,Cha, Yujin,Athul,Bhuniya, Sankarprasad,Lee, Min Hee
, p. 9614 - 9617 (2021)
The endogenous H2S-driven theranosticH2S-Gemhas been invented. The theranostic prodrugH2S-Gemis selectively activated in cancer cells, releasing active gemcitabine with a simultaneous fluorescence turn-on.H2S-Gemselectively inhibited cancer cell growth compared to the mother chemotherapeutic gemcitabine. Overall, it is a unique protocol for tracking and transporting chemotherapeutic agents to tumor areas without the guidance of tumor-directive ligands.
Exploring boron applications in modern agriculture: A structure-activity relationship study of a novel series of multi-substitution benzoxaboroles for identification of potential fungicides
Liu, Chunliang,Steere, Luke,McGregor, Cari,Frederick, Brittany H.,Pastoor, Timothy,Zhou, Yasheen,Liu, C. Tony,Cai, Yan,Zhou, Haibo,Xu, Musheng,Wang, Jiangong,Kim, Sang Hu,Whitesell, Luke,Cowen, Leah E.,Zhang, Yong-Kang
, (2021/05/19)
Several boron-containing small molecules have been approved by the US FDA to treat human diseases. We explored potential applications of boron-containing compounds in modern agriculture by pursuing multiple research and development programs. Here, we report a novel series of multi-substitution benzoxaboroles (1–36), a compound class that we recently reported as targeting geranylgeranyl transferase I (GGTase I) and thereby inhibiting protein prenylation (Kim et al., 2020). These compounds were designed, synthesized, and tested against the agriculturally important fungal pathogens Mycosphaerella fijiensis and Colletotrichum sublineolum in a structure–activity relationship (SAR) study. Compounds 13, 28, 30, 34 and 36 were identified as active leads with excellent antifungal MIC95 values in the range of 1.56–3.13 ppm against M. fijiensis and 0.78–3.13 ppm against C. sublineolum.
Bypassing Biocatalytic Substrate Limitations in Oxidative Dearomatization Reactions by Transient Substrate Mimicking
Milzarek, Tobias M.,Einsiedler, Manuel,Aldemir, Hülya,D'Agostino, Paul M.,Evers, Julia K.,Hertrampf, Gesa,Lamm, Katharina,Malay, Mert,Matura, Anke,Müller, Jonas I.,Gulder, Tobias A. M.
supporting information, p. 4520 - 4524 (2019/06/27)
Enzymatic oxidative dearomatization is an efficient way to generate chiral molecules from simple arenes. One example is the flavin-dependent monooxygenase SorbC involved in sorbicillinoid biosynthesis. However, SorbC requires a long-chain keto substituent at its phenolic substrate, thus preventing its application beyond the synthesis of natural sorbicillinoids or close structural analogues. This work describes an approach to broaden the accessible product spectrum of SorbC by employing an ester functionality mimicking the natural substrate structure during enzymatic oxidation.