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Pharmacological profiling of novel non-COX-inhibiting indole-pyran analogues of etodolac reveals high solid tumour activity of SDX-308 in vitro
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Medical Sciences. (Cancer Pharmacology and Informatics)
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Medical Sciences. (Cancer Pharmacology and Informatics)
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2007 (English)In: Investigational new drugs, ISSN 0167-6997, E-ISSN 1573-0646, Vol. 25, no 4, 297-303 p.Article in journal (Refereed) Published
Abstract [en]

SDX-308 and SDX-309 are potent indole-pyran analogues of SDX-101 (R-etodolac) which has anti-tumour activity unrelated to cyclooxygenase-2 inhibition. Their cytotoxic activity was further studied herein using a well-characterized human tumour cell-line panel containing ten cell lines, as well as in 58 primary tumour cell samples from a variety of diagnoses. The indole-pyran analogues of SDX-101 were in general considerably more active in both cancer cell lines and primary tumour samples. Low cross-reactivity with standard agents was observed, indicating a unique mechanism of action. No apparent influence on efficacy was observed via classical mechanisms of multidrug-resistance. SDX-101 and SDX-309 showed higher relative activity in haematological compared to solid tumour samples, while SDX-308 had pronounced solid-tumour activity. High SDX-308 cytotoxic efficacy was observed in non-small cell lung cancer, renal cancer and ovarian cancer samples, and also in chronic lymphocytic leukaemia. In conclusion, the indole-pyran analogues showed a favourable pharmacological profile and represent a potentially important new class of drugs for cancer treatment.

Place, publisher, year, edition, pages
2007. Vol. 25, no 4, 297-303 p.
Keyword [en]
Antineoplastic Agents/*pharmacology, Cell Line; Tumor, Drug Screening Assays; Antitumor, Etodolac/*analogs & derivatives/*pharmacology, Female, Heterocyclic Compounds; 3-Ring/*pharmacology, Humans
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Medical and Health Sciences
URN: urn:nbn:se:uu:diva-15630DOI: 10.1007/s10637-007-9049-4ISI: 000247275600002PubMedID: 17440681OAI: oai:DiVA.org:uu-15630DiVA: diva2:43401
Available from: 2008-02-26 Created: 2008-02-26 Last updated: 2011-02-05Bibliographically approved

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Lindhagen, ElinRickardson, LindaNygren, PeterLarsson, RolfÅleskog, Anna
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Department of Medical SciencesDepartment of Oncology, Radiology and Clinical Immunology
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