Although taxanes such as paclitaxel and docetaxel are the two most important clinically available anticancer drugs for the treatment of various cancers (including colon cancer), the success of these two drugs has been tempered by the development of various unbearable side effects as well as multi-drug resistance. Therefore, it is essential to search new taxane analogues with improved anticancer activity and fewer side effects to gain the maximum benefits for colon cancer patients. In this paper, four series of taxane derivatives were used to correlate their inhibitory activities against colon cancers mainly with the hydrophobic and steric descriptors of their substituents in order to gain a better understanding of their chemical-biological interactions. QSAR results from this paper have suggested that the steric and hydrophobic parameters of the substituents are the two most important determinants for the activities of taxane analogues (under consideration) against colon cancers, with a major contribution coming from the molar refractivity of the substituents. Statistical diagnostics, internal validation, and external validation tests have validated all the QSAR models.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2009.12.054 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Chemotherapy and radiotherapy for advanced pancreatic cancer.
Cochrane Database Syst Rev
December 2024
Medical Oncology, The Kinghorn Cancer Care Centre, St Vincent's Hospital, Sydney, Australia.
Article Synopsis
- Pancreatic cancer is a highly lethal disease with limited treatment options, leading to an updated review of randomized data focused on first-line treatments for advanced cases.
- The review examines the impact of chemotherapy, radiotherapy, or a combination of both on overall survival, severe adverse events, and quality of life for patients with unresectable or metastatic pancreatic cancer.
- A total of 75 studies were analyzed, with 51 included in the meta-analysis, examining various treatment comparisons and finding that the studies generally had low risks for biases in methodology.
Pelophen B is a non-taxoid binding microtubule-stabilizing agent with promising preclinical anticancer properties.
Sci Rep
December 2024
Laboratory of Experimental Cancer Research, Department of Human Structure and Repair, Ghent University, Ghent, Belgium.
Taxanes, such as paclitaxel (PTX), stabilize microtubules and are used as a first-line therapy in multiple cancer types. Disruption of microtubule equilibrium, which plays an essential role in mitosis and cell homeostasis, ultimately results in cell death. Even though PTX is a very potent chemotherapy, its use is associated with major side effects and therapy resistance.
View Article and Find Full Text PDF[A real-world study of first-line albumin-bound paclitaxel in the treatment of advanced pancreatic cancer in China].
Zhonghua Zhong Liu Za Zhi
November 2024
Department of Oncology, Nanjing Drum Tower Hospital, Affiliated Hospital of Medical School, Nanjing University, Nanjing210008, China.
To observe and evaluate the clinical efficacy and safety of albumin-bound paclitaxel as first-line treatment for patients with advanced pancreatic cancer in China, and to explore the prognosis-related molecules in pancreatic cancer based on next-generation sequencing (NGS) of tumor tissues. From December 2018 to December 2020, patients with locally advanced or metastatic pancreatic cancer were recruited to accept albumin-bound paclitaxel as first-line treatment in the oncology departments of 24 hospitals in East China. The primary endpoints were overall survival (OS) and treatment related adverse events, and the secondary endpoint was progression-free survival (PFS).
View Article and Find Full Text PDFMg-Ion Dependence Revealed for a BAHD 13--β-Aminoacyltransferase from Plants.
JACS Au
November 2024
Department of Chemistry, Michigan State University, East Lansing, Michigan 48824, United States.
A baccatin III:3-amino-3-phenylpropanoyltransferase (BAPT, Accession: AY082804) in clade 6 of the BAHD family catalyzed a Mg-dependent transfer of isoserines from their corresponding CoA thioesters. An advanced taxane baccatin III on the paclitaxel biosynthetic pathway in plants was incubated BAPT and phenylisoserine CoA or isobutenylisoserinyl CoA with and without MgCl. BAPT biocatalytically converted baccatin III to its 13--phenylisoserinyl and 3-(1',1'-dimethylvinyl)isoserinyl analogs, an activity that abrogated when Mg ions were omitted.
View Article and Find Full Text PDFInduction chemotherapy for locally advanced nasopharyngeal carcinoma: Efficacy and safety of the TPC regimen compared to GP and TPF.
Oral Oncol
January 2025
Department of Radiation Oncology, Guangxi Medical University Cancer Hospital, Nanning, Guangxi 530021, China; Department of Oncology, Wuming Hospital of Guangxi Medical University, Nanning, Guangxi 530199, China. Electronic address:
Background And Objectives: Gemcitabine plus cisplatin (GP) and docetaxel plus cisplatin plus fluorouracil (TPF) are induction chemotherapy (IC) regimens for locally advanced nasopharyngeal carcinoma (LA-NPC). The oral convenience of capecitabine presents its potential as a fluorouracil substitute in the TPF regimen, which has yet to be thoroughly investigated. This study aims to compare the efficacy and safety of the docetaxel, cisplatin, and capecitabine (TPC) with GP and TPF in LA-NPC.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!