Synthesis of the 1,5-disubstituted tetrazole-methanesulfonylindole hybrid system via high-order multicomponent reaction

• Cesia M. Aguilar-Morales,
• América A. Frías-López,
• Nadia V. Emilio-Velázquez,
• Alejandro Islas-Jácome,
• Angelica Judith Granados-López,
• Jorge Gustavo Araujo-Huitrado,
• Yamilé López-Hernández,
• Hiram Hernández-López,
• Luis Chacón-García,
• Jesús Adrián López and
• Carlos J. Cortés-García

Beilstein J. Org. Chem. 2024, 20, 3077–3084, doi:10.3762/bjoc.20.256

• ; isocyanides; MCF-7 cell line; methanesulfonylindoles; Ugi-azide reaction; Introduction Nitrogen-containing heterocyclic moieties, such as 1,5-disubstituted tetrazoles and indoles, are considered pharmacophoric fragments due to their pivotal interactions with several targets involved in many diseases. They

• against MCF-7 cell line, which has been used as a model for breast cancer (BC), a public health issue very common and a deadly pathology worldwide, where women between 45 and 55 years of age are the most vulnerable population. In 2020, 684,996 deaths were recorded [40][41][42][43]. This in vitro

• compounds that elicited proliferation inhibition are ordered below from the highest to lowest effect on MCF-7 cell line: 18d, 18j, 18h, 18i, 18b, 18f, 18a, 18g, 18c, and 18e. Compounds 18c, and 18e did not affect MCF-7 cell proliferation inhibition. Regarding the structure–activity relationship, the

Formulation development, stability and anticancer efficacy of core-shell cyclodextrin nanocapsules for oral chemotherapy with camptothecin

• Hale Ünal,
• Naile Öztürk and
• Erem Bilensoy

Beilstein J. Org. Chem. 2015, 11, 204–212, doi:10.3762/bjoc.11.22

• suggesting the improved protection of the drug molecule from rapid hydrolysis degradation or gastrointestinal pH in nanocapsule oily core. Furthermore CD nanocapsules showed higher anticancer efficacy than CPT solution against the MCF-7 cell line. Permeation of CPT across Caco-2 cells was found to be 3 fold

• concentration of 3.125 µg/mL (see Supporting Information File 1 for full experimental data). The incubation time is depending on both the doubling time of the MCF-7 cell line and the release characteristics of the formulations. The MCF-7 cell line has a doubling time over 38 h and CPT was released from