[HTML][HTML] Target-based anticancer indole derivatives and insight into structure‒activity relationship: A mechanistic review update (2018–2021)

A Dhiman, R Sharma, RK Singh - Acta Pharmaceutica Sinica B, 2022 - Elsevier
Cancer, which is the uncontrolled growth of cells, is the second leading cause of death after
heart disease. Targeting drugs, especially to specific genes and proteins involved in growth …

Current scenario of indole derivatives with potential anti-drug-resistant cancer activity

Y Jia, X Wen, Y Gong, X Wang - European Journal of Medicinal Chemistry, 2020 - Elsevier
Cancer chemotherapy is frequently hampered by drug resistance, so the resistance to
anticancer agents represents one of the major obstacles for the effective cancer treatment …

Thiazole-based thiosemicarbazones: Synthesis, cytotoxicity evaluation and molecular docking study

SM Gomha, HA Abdelhady, DZH Hassain… - Drug design …, 2021 - Taylor & Francis
Introduction Hybrid drug design has developed as a prime method for the development of
novel anticancer therapies that can theoretically solve much of the pharmacokinetic …

1, 2, 4-Amino-triazine derivatives as pyruvate dehydrogenase kinase inhibitors: Synthesis and pharmacological evaluation

C Pecoraro, M De Franco, D Carbone… - European Journal of …, 2023 - Elsevier
Among the different hallmarks of cancer, deregulation of cellular metabolism turned out to be
an essential mechanism in promoting cancer resistance and progression. The pyruvate …

1, 2, 4-Oxadiazole topsentin analogs as staphylococcal biofilm inhibitors targeting the bacterial transpeptidase sortase A

B Parrino, D Carbone, S Cascioferro… - European journal of …, 2021 - Elsevier
The inhibition or prevention of biofilm formation represents an emerging strategy in the war
against antibiotic resistance, interfering with key players in bacterial virulence. This …

Discovery of the 3-amino-1, 2, 4-triazine-based library as selective PDK1 inhibitors with therapeutic potential in highly aggressive pancreatic ductal adenocarcinoma

D Carbone, M De Franco, C Pecoraro… - International Journal of …, 2023 - mdpi.com
Pyruvate dehydrogenase kinases (PDKs) are serine/threonine kinases, that are directly
involved in altered cancer cell metabolism, resulting in cancer aggressiveness and …

Thiadiazole derivatives as anticancer agents

M Szeliga - Pharmacological Reports, 2020 - Springer
In spite of substantial progress made toward understanding cancer pathogenesis, this
disease remains one of the leading causes of mortality. Thus, there is an urgent need to …

[PDF][PDF] CHK1 inhibitor sensitizes resistant colorectal cancer stem cells to nortopsentin

S Di Franco, B Parrino, M Gaggianesi, VD Pantina… - Iscience, 2021 - cell.com
Limited therapeutic options are available for advanced colorectal cancer (CRC). Herein, we
report that exposure to a neo-synthetic bis (indolyl) thiazole alkaloid analog, nortopsentin …

Intermolecular C–H Aminocyanation of Indoles via Copper–iodine Cocatalyzed Tandem C–N/C–C Bond Formation

W Yu, X Zhang, C Liu, Y Zhang, X Gu… - The Journal of …, 2022 - ACS Publications
An efficient copper–iodine cocatalyzed intermolecular C–H aminocyanation of indoles with a
broad substrate scope has been developed for the first time. This method enables highly …

Structural manipulations of marine natural products inspire a new library of 3-amino-1, 2, 4-triazine PDK inhibitors endowed with antitumor activity in pancreatic ductal …

D Carbone, M De Franco, C Pecoraro, D Bassani… - Marine Drugs, 2023 - mdpi.com
Pancreatic ductal adenocarcinoma (PDAC) is one of the main aggressive types of cancer,
characterized by late prognosis and drug resistance. Among the main factors sustaining …