STUDY ON ANTI CANCER ACTIVITY OF DIFFERENT 2-

PYRIDINEFORMAMIDE THIOSEMICARBAZONE DERIVATIVE

COMPOUNDS ON HeLa CELLS

Central Department of
Biotechnology
Introduction
• Cancer remains one of the most challenging health issues worldwide,
characterized by uncontrolled cellular growth, invasion, and potential
metastasis. (Geoffrey M. Cooper, 2019).
• Amidst this medical landscape, the potential of thiosemicarbazones
and their derivatives in cancer therapy has garnered significant
attention. (Heiner et al., 1971).
• Thiosemicarbazones, represented by the chemical formula
H2NC(S)NHN=CR2, have been extensively researched for their
diverse biological activities, notably in combating bacteria, viruses,
malaria, and tumors. (Wattanakanjana et al., 2012)
Thiosemicarbazones and their Derivatives:
• Thiosemicarbazones exhibit antimicrobial effects and have showcased
antiviral properties since the 1940s.
• Their capabilities expanded into cancer research, notably with
pyridine-2-carboxaldehyde thiosemicarbazone, displaying promising
results in extending the lifespan of mice with leukemia. (Shakya et al.,
2019)

Figure 1 Preparation pathway of 2-pyridineformamide

thiosemicarbazone and its derivatives (Shakya et al., 2019)
Ribonucleotide Reductase (RNR)
• The crucial role of RNR in DNA synthesis and cell growth regulation is
pivotal. (Herrick & Sclavi, 2007).
• Inhibitors, particularly α-(N)-heterocyclic thiosemicarbazones, disrupt
RNR activity, impeding cancer cell proliferation and serving as
potential anti-cancer agents. (Colleen Moore & Sartorelli, 1984).
Cancer Pathogenesis
• The progression from normal to cancerous cells involves a series of
genetic changes that promote uncontrolled growth, invasion, and
metastasis.
• Understanding these alterations is crucial in identifying effective
therapeutic targets(Harvey Lodish, 2016)
The MTT Assay
• Methodologies such as the MTT assay offer a means to evaluate
cellular metabolic activity and potential viability.
• The MTT assay principle relies on the conversion of the MTT reagent
into insoluble formazan by metabolically active cells. This formazan is
measured spectrophotometrically to determine cell metabolic activity
or viability. (Ghasemi et al., 2021)

Reduction of MTT to formazan crystal (Kamiloglu et al., 2020)