150099-69-7Relevant articles and documents
Near-IR-triggered, remote-controlled release of metal ions: A novel strategy for caged ions
Atilgan, Ahmet,Tanriverdi E?ik, Esra,Guliyev, Ruslan,Uyar, T. Bilal,Erbas-Cakmak, Sundus,Akkaya, Engin U.
, p. 10678 - 10681 (2014)
A ligand incorporating a dithioethenyl moiety is cleaved into fragments which have a lower metal-ion affinity upon irradiation with low-energy red/near-IR light. The cleavage is a result of singlet oxygen generation which occurs on excitation of the photosensitizer modules. The method has many tunable factors that could make it a satisfactory caging strategy for metal ions. Metal ions on demand: Near-IR irradiation of a designer ligand results in singlet-oxygen-mediated fragmentation with the consequent release of metal ions. The modular nature of the "cage" may herald a new class of agents that could supply chemical effectors on demand.
Second-generation testosterone-platinum(II) hybrids for site-specific treatment of androgen receptor positive prostate cancer: Design, synthesis and antiproliferative activity
Ouellette, Vincent,C?té, Marie-France,Gaudreault, René C.,Tajmir-Riahi, Heidar-Ali,Bérubé, Gervais
, p. 660 - 666 (2019)
Prostate cancer is the most diagnosed type of cancer in men in Canada. One out of eight men will be stricken with this disease during the course of his life. It is noteworthy that, at initial diagnoses 80–90% of cancers are androgen dependent. Hence, the androgen receptor is a viable biological target to be considered for drug targeting. We have developed a new generation of testosterone-Pt(II) hybrids for site-specific treatment of hormone-dependent prostate cancer. The hybrid molecules are made from testosterone using an eight-step reaction sequence with about 7% overall yield. They are linked with a stronger tether chain between the testosterone moiety and the Pt(II) moiety in comparison to our first generation hybrids. The new hybrids were tested on hormone-dependent and –independent prostate cancer cell lines. The hybrid 3a presents the best antiproliferative activity and was selective on hormone-dependent prostate cancer with IC50 of 2.2 μM on LNCaP (AR+) in comparison to 13.3 μM on PC3 (AR-) and 8.8 μM on DU145 (AR-) prostate cancer cells. On the same cell lines, CDDP displayed IC50 of 2.1 μM, 0.5 μM and 1.0 μM, respectively. Remarkably, hybrid 3a was inactive on both colon carcinoma (HT-29) and normal human adult keratinocyte cells (HaCat) with an IC50 of >25 μM. This is not the case for CDDP showing IC50 of 1.3 μM and 5.1 μM on HT-29 and HaCat cells, respectively. The potential for selective activity on androgen-receptor positive prostate cancer cells is confirmed with hybrid 3a giving new hope for an efficient and less toxic platinum-based treatment of prostate cancer patients.
Redox-Neutral Metal-Free Three-Component Carbonylative Dearomatization of Pyridine Derivatives with CO2
Cerveri, Alessandro,Pace, Stefano,Monari, Magda,Lombardo, Marco,Bandini, Marco
supporting information, p. 15272 - 15276 (2019/11/19)
The TBD (1,3,5-triazabicyclodec-5-ene) assisted three-component carbonylation of pyridine-2-methanamines is documented by means of CO2 as a benign CO surrogate. The redox-neutral methodology enables the realization of densely functionalized imi
